ketoconazole

Summary

Summary: Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.

Top Publications

  1. ncbi Lack of significant effect of bilastine administered at therapeutic and supratherapeutic doses and concomitantly with ketoconazole on ventricular repolarization: results of a thorough QT study (TQTS) with QT-concentration analysis
    Benoit Tyl
    Robert Ballanger s Hospital, Department of Cardiology, Aulnay sous Bois, France
    J Clin Pharmacol 52:893-903. 2012
  2. pmc 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
    Charles J Ryan
    Urologic Oncology Program, University of California, San Francisco, San Francisco, CA 94115, USA
    J Clin Oncol 28:1481-8. 2010
  3. ncbi Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole
    H Huang
    Albert Einstein Cancer Center, Albert Einstein College of Medicine, Bronx, NY 10461, USA
    Oncogene 26:258-68. 2007
  4. ncbi In vivo effects of cyclosporin A and ketoconazole on the pharmacokinetics of representative substrates for P-glycoprotein and cytochrome P450 (CYP) 3A in rats
    Michiharu Kageyama
    Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina ku, Kyoto 607 8414, Japan
    Biol Pharm Bull 28:316-22. 2005
  5. ncbi Stochastic prediction of CYP3A-mediated inhibition of midazolam clearance by ketoconazole
    Jenny Y Chien
    Department of Drug Disposition, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 34:1208-19. 2006
  6. ncbi Melanin biosynthesis in Madurella mycetomatis and its effect on susceptibility to itraconazole and ketoconazole
    Wendy W J van de Sande
    Erasmus MC, University Medical Centre Rotterdam, Department of Medical Microbiology and Infectious Diseases, Dr Molewaterplein 40, 3015 GD Rotterdam, The Netherlands
    Microbes Infect 9:1114-23. 2007
  7. ncbi Cytochrome P450 3A4 inhibition by ketoconazole: tackling the problem of ligand cooperativity using molecular dynamics simulations and free-energy calculations
    Urban Bren
    Institute of Molecular Modeling and Simulation, University of Natural Resources and Life Sciences, Muthgasse 18, AT 1190 Vienna, Austria
    J Chem Inf Model 52:1573-82. 2012
  8. ncbi Induction of cytochrome P450 1A1 by ketoconazole and itraconazole but not fluconazole in murine and human hepatoma cell lines
    Hesham M Korashy
    Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada T6G 2N8
    Toxicol Sci 97:32-43. 2007
  9. ncbi Cyclosporin and ketoconazole interaction for treatment of perianal fistulas in the dog
    J G Mouatt
    Veterinary Teaching Hospital, University of Queensland, St Lucia
    Aust Vet J 80:207-11. 2002
  10. ncbi Cytochrome P450 3A4 in vivo ketoconazole competitive inhibition: determination of Ki and dangers associated with high clearance drugs in general
    H Boxenbaum
    Arishel Inc, North Potomac, Maryland, USA
    J Pharm Pharm Sci 2:47-52. 1999

Research Grants

Detail Information

Publications332 found, 100 shown here

  1. ncbi Lack of significant effect of bilastine administered at therapeutic and supratherapeutic doses and concomitantly with ketoconazole on ventricular repolarization: results of a thorough QT study (TQTS) with QT-concentration analysis
    Benoit Tyl
    Robert Ballanger s Hospital, Department of Cardiology, Aulnay sous Bois, France
    J Clin Pharmacol 52:893-903. 2012
    ..and supratherapeutic doses (20 mg and 100 mg once daily, respectively), and bilastine 20 mg administered with ketoconazole 400 mg...
  2. pmc 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
    Charles J Ryan
    Urologic Oncology Program, University of California, San Francisco, San Francisco, CA 94115, USA
    J Clin Oncol 28:1481-8. 2010
    ..This phase I dose-escalation study of abiraterone acetate evaluated safety, pharmacokinetics, and effects on steroidogenesis and prostate-specific antigen (PSA) levels in men with CPRC with or without prior ketoconazole therapy.
  3. ncbi Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole
    H Huang
    Albert Einstein Cancer Center, Albert Einstein College of Medicine, Bronx, NY 10461, USA
    Oncogene 26:258-68. 2007
    ..We have found that xenobiotic-mediated induction of CYP3A4 and MDR-1 gene transcription was inhibited by ketoconazole, a commonly used antifungal drug...
  4. ncbi In vivo effects of cyclosporin A and ketoconazole on the pharmacokinetics of representative substrates for P-glycoprotein and cytochrome P450 (CYP) 3A in rats
    Michiharu Kageyama
    Department of Pharmacokinetics, Kyoto Pharmaceutical University, Yamashina ku, Kyoto 607 8414, Japan
    Biol Pharm Bull 28:316-22. 2005
    In this study, the in vivo effects of cyclosporin A (CsA) and ketoconazole (KCZ), which are used as inhibitors of P-glycoprotein (Pgp) and cytochrome P450 (CYP) 3A, respectively, on the pharmacokinetics of rhodamine 123 (Rho123), ..
  5. ncbi Stochastic prediction of CYP3A-mediated inhibition of midazolam clearance by ketoconazole
    Jenny Y Chien
    Department of Drug Disposition, Lilly Research Laboratories, Indianapolis, IN 46285, USA
    Drug Metab Dispos 34:1208-19. 2006
    ..A physiologically based PK model was developed to predict the inhibition of CYP3A by ketoconazole (KTZ), using midazolam (MDZ) as the substrate...
  6. ncbi Melanin biosynthesis in Madurella mycetomatis and its effect on susceptibility to itraconazole and ketoconazole
    Wendy W J van de Sande
    Erasmus MC, University Medical Centre Rotterdam, Department of Medical Microbiology and Infectious Diseases, Dr Molewaterplein 40, 3015 GD Rotterdam, The Netherlands
    Microbes Infect 9:1114-23. 2007
    ..added to the culture medium, MICs were found to be 16-fold elevated in the case of itraconazole and 32-fold for ketoconazole. MICs for amphotericin B, fluconazole and voriconazole were not affected...
  7. ncbi Cytochrome P450 3A4 inhibition by ketoconazole: tackling the problem of ligand cooperativity using molecular dynamics simulations and free-energy calculations
    Urban Bren
    Institute of Molecular Modeling and Simulation, University of Natural Resources and Life Sciences, Muthgasse 18, AT 1190 Vienna, Austria
    J Chem Inf Model 52:1573-82. 2012
    ..was applied to elucidate the physicochemical origin of the observed positive homotropic cooperativity in ketoconazole binding to CYP3A4...
  8. ncbi Induction of cytochrome P450 1A1 by ketoconazole and itraconazole but not fluconazole in murine and human hepatoma cell lines
    Hesham M Korashy
    Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada T6G 2N8
    Toxicol Sci 97:32-43. 2007
    ..Therefore, we examined here the ability of three structurally different antifungal drugs, ketoconazole (KTZ), itraconazole (ITZ), and fluconazole (FLZ) to induce the CYP1A1, an enzyme known to play an important ..
  9. ncbi Cyclosporin and ketoconazole interaction for treatment of perianal fistulas in the dog
    J G Mouatt
    Veterinary Teaching Hospital, University of Queensland, St Lucia
    Aust Vet J 80:207-11. 2002
    To assess the use of concurrent ketoconazole and low dose cyclosporin administration in a group of dogs with clinical evidence of perianal fistulas, and to determine if this combination could be used to manage perianal fistulas effectively...
  10. ncbi Cytochrome P450 3A4 in vivo ketoconazole competitive inhibition: determination of Ki and dangers associated with high clearance drugs in general
    H Boxenbaum
    Arishel Inc, North Potomac, Maryland, USA
    J Pharm Pharm Sci 2:47-52. 1999
    ..When triazolam is the P450 3A4 substrate and ketoconazole the competitive inhibitor, Ki approximately 1.2 microg/mL in humans...
  11. ncbi Anticandidal effect of Ocimum sanctum essential oil and its synergy with fluconazole and ketoconazole
    K Amber
    Department of Biosciences, Jamia Millia Islamia, New Delhi, India
    Phytomedicine 17:921-5. 2010
    ..antifungal effect of Ocimum sanctum essential oil (OSEO) and established azole antimycotics-fluconazole and ketoconazole. To put forward this approach, antifungal activity has been assessed in seventy four fluconazole-sensitive and ..
  12. ncbi Randomized trial with itraconazole, ketoconazole and sulfadiazine in paracoccidioidomycosis
    M A Shikanai-Yasuda
    Department of Infectious and Parasitic Diseases, School of Medicine, Sao Paulo University, Brazil
    Med Mycol 40:411-7. 2002
    Forty-two patients with active paracoccidioidomycosis were randomized to receive itraconazole (50-100 mg d(-1)), ketoconazole (200-400 mg d(-1)) or sulfadiazine (100-150 mg kg d(-1) up to 6 g d(-1)) for 4-6 months, followed by slow ..
  13. pmc Contemporary experience with ketoconazole in patients with metastatic castration-resistant prostate cancer: clinical factors associated with PSA response and disease progression
    Daniel Keizman
    The Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins School of Medicine, Baltimore, Maryland, USA
    Prostate 72:461-7. 2012
    ..Compounds targeting CYP-17 hydroxylase and lyase, as ketoconazole and abiraterone, block adrenal/intratumoral androgen biosynthesis, and are used as sequential endocrine ..
  14. ncbi The effect of ketoconazole on whole blood and skin ciclosporin concentrations in dogs
    Laura L Gray
    Department of Veterinary Clinical Sciences, College of Veterinary Medicine, The Ohio State University, Columbus, OH 43210, USA
    Vet Dermatol 24:118-25.e27-8. 2013
    Ciclosporin (CSA) is approved for the treatment of canine atopic dermatitis. Ciclosporin is metabolized by liver cytochrome P450 enzymes, a process inhibited by ketoconazole (KTZ).
  15. ncbi Efficacy of combined cyclosporine A and ketoconazole treatment of anal furunculosis
    T O'Neill
    Small Animal Hospital, University of Liverpool, Crown Street, Liverpool L7 7EX
    J Small Anim Pract 45:238-43. 2004
    Cyclosporine A and ketoconazole were used as a combined therapy to treat 19 dogs with anal furunculosis. Complete resolution of all lesions was achieved in three to 10 weeks, but recurrences occurred in seven of the 19 dogs (36...
  16. ncbi Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants
    Chiaki Tanaka
    Oncology Clinical Pharmacology, Novartis Pharmaceuticals Corporation, 180 Park Ave, Florham Park, NJ 07932, USA
    J Clin Pharmacol 51:75-83. 2011
    ..conducted in healthy volunteers prior to and following treatment with a strong inducer (rifampin) or inhibitor (ketoconazole)...
  17. ncbi Synthesis of novel brassinosteroid biosynthesis inhibitors based on the ketoconazole scaffold
    Keimei Oh
    Department of Biotechnology, Faculty of Bioresource Sciences, Akita Prefectural University, Nakano, Akita, Japan
    Bioorg Med Chem Lett 22:1625-8. 2012
    ..We synthesized novel triazole derivatives, based on the ketoconazole scaffold, that function as inhibitors of BR biosynthesis...
  18. ncbi Effect of ketoconazole on the pharmacokinetics of oral bosutinib in healthy subjects
    Richat Abbas
    Pfizer Inc, Collegeville, PA 19426, USA
    J Clin Pharmacol 51:1721-7. 2011
    ..The effect of coadministration of ketoconazole on the pharmacokinetic (PK) profile of bosutinib was evaluated in an open-label, randomized, 2-period, ..
  19. ncbi Activity of dutasteride plus ketoconazole in castration-refractory prostate cancer after progression on ketoconazole alone
    Oliver Sartor
    Dana Farber Cancer Institute, Boston, MA, USA
    Clin Genitourin Cancer 7:E90-2. 2009
    b>Ketoconazole is a commonly used secondary hormonal therapy in castration-refractory prostate cancer (CRPC), but disease progression inevitably occurs...
  20. ncbi Comparison of abiraterone acetate versus ketoconazole in patients with metastatic castration resistant prostate cancer refractory to docetaxel
    Avivit Peer
    Department of Oncology, Rambam Medical Center, Haifa, Israel
    Prostate 74:433-40. 2014
    ..However, in countries where abiraterone has not been approved yet, or for patients who cannot afford it, ketoconazole is used as an alternative CYP 17 inhibitor...
  21. ncbi Adrenal androgen levels as predictors of outcome in prostate cancer patients treated with ketoconazole plus antiandrogen withdrawal: results from a cancer and leukemia group B study
    Charles J Ryan
    Urologic Oncology Program, University of California, San Francisco, California 94143, USA
    Clin Cancer Res 13:2030-7. 2007
    Adrenal androgens activate the androgen receptor and stimulate prostate cancer growth. Ketoconazole is used as an inhibitor of adrenal androgen synthesis in men with androgen-independent prostate cancer...
  22. ncbi Alteration of lipid order profile and permeability of plasma membranes from Trypanosoma cruzi epimastigotes grown in the presence of ketoconazole
    J A Urbina
    Centro de Biologia Celular, Facultad de Ciencias, Universidad Central de Venezuela, Caracas
    Mol Biochem Parasitol 30:185-95. 1988
    Highly purified preparations of plasma membranes from control and ketoconazole-treated (1 microM, 120 h) epimastigotes of Trypanosoma cruzi have been obtained by cell disruption using abrasion with glass beads, differential centrifugation ..
  23. ncbi Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers
    Annika Allqvist
    Karolinska Institutet, Department of Laboratory Medicine, Division of Clinical Pharmacology at Karolinska University Hospital, Huddinge, Stockholm, Sweden
    Eur J Clin Pharmacol 63:173-9. 2007
    The antifungal drug ketoconazole (KTZ) is known as an inhibitor of, especially, the CYP3A subfamily, which catalyzes the metabolism of a large variety of drugs...
  24. ncbi A phase II clinical trial of neoadjuvant ketoconazole and docetaxel chemotherapy before radical prostatectomy in high risk patients
    Paul R Womble
    Department of Urology, University of Kansas Hospital, University of Kansas Medical Center, Kansas City, Kansas 66160, USA
    J Urol 186:882-7. 2011
    ..Looking for improvement on these outcomes, we conducted a phase II clinical trial examining the combination of ketoconazole and docetaxel in the neoadjuvant setting before radical prostatectomy.
  25. ncbi Enantioselectivity of inhibition of cytochrome P450 3A4 (CYP3A4) by ketoconazole: Testosterone and methadone as substrates
    Shahrzad Dilmaghanian
    Division of Clinical Pharmacology and Toxicology, University of Colorado Health Sciences Center, Denver, Colorado, USA
    Chirality 16:79-85. 2004
    Racemic ketoconazole (KTZ) was the first orally active azole antifungal agent used in clinical practice and has become widely used in the treatment of mucosal fungal infections associated with AIDS immunosuppression and cancer ..
  26. ncbi Effectiveness of cabergoline in monotherapy and combined with ketoconazole in the management of Cushing's disease
    Lucio Vilar
    Division of Endocrinology, Hospital das Clinicas, Federal University of Pernambuco, Recife, Brazil
    Pituitary 13:123-9. 2010
    ..the effectiveness of cabergoline (at doses of up 3 mg/week), alone or combined with relatively low doses of ketoconazole (up to 400 mg/day), in 12 patients with CD unsuccessfully treated by transsphenoidal surgery...
  27. ncbi Antifungal activity of the essential oil of Agastache rugosa Kuntze and its synergism with ketoconazole
    S Shin
    College of Pharmacy, Duksung Women s University, Ssangmoondong 419, Dobongku, Seoul, Korea
    Lett Appl Microbiol 36:111-5. 2003
    To evaluate the fungitoxic activity of the essential oil of Agastache rugosa alone and to determine its combination effect with ketoconazole against Blastoschizomyces capitatus.
  28. ncbi Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP)
    Anshul Gupta
    Department of Pharmaceutics, School of Pharmacy, University of Washington, Seattle, WA 98195 7610, USA
    J Pharm Sci 96:3226-35. 2007
    ..The goal of this study was to investigate the interactions of azole antifungal agents, ketoconazole, itraconazole, fluconazole, and voriconazole, with BCRP...
  29. ncbi Administration of high-dose ketoconazole, an inhibitor of steroid synthesis, prevents posttraumatic anxiety in an animal model
    H Cohen
    Ministry of Health, Beer Sheva Mental Health Center, Anxiety and Stress Research Unit, P O 4600, Beer Sheva, Israel
    Eur Neuropsychopharmacol 10:429-35. 2000
    ..b>Ketoconazole (KTCZ), an imidazole derivative, is a potent inhibitor of gonadal and adrenal steroidogenesis...
  30. ncbi Ketoconazole increases fingolimod blood levels in a drug interaction via CYP4F2 inhibition
    John M Kovarik
    Novartis Pharma, Building WSJ 210 427, 4002 Basel, Switzerland
    J Clin Pharmacol 49:212-8. 2009
    ..In vitro experiments showed that ketoconazole significantly inhibited the oxidative metabolism of fingolimod by human liver microsomes and by recombinant ..
  31. pmc Phase II study of androgen synthesis inhibition with ketoconazole, hydrocortisone, and dutasteride in asymptomatic castration-resistant prostate cancer
    Mary Ellen Taplin
    Beth Israel Deaconess Medical Center, 330 Brookline Avenue, Boston, MA 02115, USA
    Clin Cancer Res 15:7099-105. 2009
    ..was designed to assess responses to blocking multiple steps in androgen synthesis with inhibitors of CYP17A1 (ketoconazole) and type I and II 5alpha-reductases (dutasteride) in patients with castration-resistant prostate cancer (CRPC).
  32. ncbi HPLC-MS/MS analysis of the products generated from all-trans-retinoic acid using recombinant human CYP26A
    James V Chithalen
    Department of Biochemistry, Queen s University, Kingston, ON, K7L 3N6, Canada
    J Lipid Res 43:1133-42. 2002
    ..Both initial and secondary metabolic steps after 4-oxo-all-trans-retinoic acid are ketoconazole-sensitive, suggesting that steps in the production of water-soluble metabolites are cytochrome P450-dependent.
  33. ncbi Antifungal effects of herbal essential oils alone and in combination with ketoconazole against Trichophyton spp
    S Shin
    College of Pharmacy, Duksung Women s University, Dobongku, Seoul, South Korea
    J Appl Microbiol 97:1289-96. 2004
    To determine the effects of herbal essential oils on Trichophyton spp. growth and to evaluate the effects of Pelargonium graveolens oil and its main components citronellol and geraniol combined with ketoconazole against Trichophyton spp.
  34. ncbi Ketoconazole revisited: a preoperative or postoperative treatment in Cushing's disease
    F Castinetti
    Department of Endocrinology, Diabetes, Metabolic Diseases and Nutrition, Hopital de la Timone, Centre Hospitalier Universitaire de Marseille and Faculté de Médecine, Universite de la Mediterranee, 264 rue St Pierre, Cedex 5, 13385 Marseille, France
    Eur J Endocrinol 158:91-9. 2008
    ..Adjunctive treatments each have specific drawbacks. Despite its inhibitory effects on steroidogenesis, the antifungal drug ketoconazole was only evaluated in series with few patients and/or short-term follow-up.
  35. ncbi In vitro susceptibility of the seven Malassezia species to ketoconazole, voriconazole, itraconazole and terbinafine
    A K Gupta
    Division of Dermatology, Department of Medicine, Sunnybrook and Women s College Health Sciences Center Sunnybrook site and the University of Toronto, Canada
    Br J Dermatol 142:758-65. 2000
    ..03-64.0 microg/mL) of three azole drugs, ketoconazole, voriconazole and itraconazole, as well as the allylamine terbinafine, using the agar dilution method...
  36. pmc A phase I clinical study of high dose ketoconazole plus weekly docetaxel for metastatic castration resistant prostate cancer
    William D Figg
    Clinical Pharmacology Program, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Urol 183:2219-26. 2010
    This phase I study of high dose ketoconazole and docetaxel was designed against castration resistant prostate cancer to determine the maximum tolerated doses, side effects, and pharmacokinetic interaction of co-administered docetaxel and ..
  37. ncbi Antiandrogen withdrawal alone or in combination with ketoconazole in androgen-independent prostate cancer patients: a phase III trial (CALGB 9583)
    Eric J Small
    UCSF Comprehensive Cancer Center, University of California San Francisco, 1600 Divisadero St, Room A 718, San Francisco, CA 94115, USA
    J Clin Oncol 22:1025-33. 2004
    ..Thereafter, adrenal androgen ablation with agents such as ketoconazole (K) is commonly utilized. The therapeutic effect of AAWD alone was compared with simultaneous AAWD and K therapy...
  38. pmc Transcriptional profiles of the response to ketoconazole and amphotericin B in Trichophyton rubrum
    Lu Yu
    State Key Laboratory for Molecular Virology and Genetic Engineering, Chinese Center for Disease Control and Prevention, Beijing 100176, China
    Antimicrob Agents Chemother 51:144-53. 2007
    Trichophyton rubrum is a pathogenic filamentous fungus of increasing medical concern. Two antifungal agents, ketoconazole (KTC) and amphotericin B (AMB), have specific activity against dermatophytes...
  39. ncbi Anti-proliferative synergy of lysophospholipid analogues and ketoconazole against Trypanosoma cruzi (Kinetoplastida: Trypanosomatidae): cellular and ultrastructural analysis
    Ricardo M Santa-Rita
    Departmento de Ultra estrutura e Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, CP 926, 21045 900, Rio de Janeiro, Brazil
    J Antimicrob Chemother 55:780-4. 2005
    Investigation of the antiproliferative synergy of the lysophospholipid analogues (LPAs) edelfosine, ilmofosine and miltefosine with the ergosterol biosynthesis inhibitor ketoconazole against Trypanosoma cruzi.
  40. ncbi Synergistic anti-candidal activity of tetrandrine on ketoconazole: an experimental study
    Hong Zhang
    Department of Dermatology, The First Affiliated Hospital, Jinan University, Guangzhou, P R China
    Planta Med 76:53-61. 2010
    ..The study examined the synergism of tetrandrine (TET) on ketoconazole (KCZ) candidacidal activity...
  41. ncbi The preventive effect of ketoconazole on experimental metastasis from a human pancreatic carcinoma may be related to its effect on prostaglandin synthesis
    George N Tzanakakis
    Department of Histology, School of Medicine, University of Crete, Heraklion, Greece
    Int J Gastrointest Cancer 32:23-30. 2002
    ..The purpose of this study was to evaluate the anti-metastatic potential of ketoconazole, a thromboxane synthetase and 5-lipoxygenase inhibitor, on hepatic metastasis from a human pancreatic ..
  42. ncbi Identification and quantitation of cis-ketoconazole impurity by capillary zone electrophoresis-mass spectrometry
    María Castro-Puyana
    Department of Analytical Chemistry, Faculty of Chemistry, University of Alcala, Ctra Madrid Barcelona Km 33 600, 28871 Alcala de Henares, Madrid, Spain
    J Chromatogr A 1114:170-7. 2006
    trans-Ketoconazole was identified and quantified as impurity of cis-ketoconazole, an antifungal compound, by capillary zone electrophoresis-electrospray-mass spectrometry (CZE-ESI-MS)...
  43. pmc The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of inhaled fluticasone furoate and vilanterol trifenatate in healthy subjects
    Rodger Kempsford
    GlaxoSmithKline R and D, Stevenage, Hertfordshire, SG1 2NY, UK
    Br J Clin Pharmacol 75:1478-87. 2013
    To investigate the effects of the cytochrome P450 3A4 (CYP3A4) inhibitor ketoconazole on the pharmacokinetics (PK) and pharmacodynamics of fluticasone furoate (FF) and vilanterol trifenatate (VI).
  44. ncbi Ketoconazole ion-exchange fiber complex: a novel method to reduce the individual difference of bioavailability in oral administration caused by gastric anacidity
    Che Xin
    School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China
    Pharm Dev Technol 18:1346-54. 2013
    ..This method is based on ion exchange of ion-exchange fibers. Water-insoluble faintly alkaline drug ketoconazole was used as a model drug...
  45. ncbi Mitotane, metyrapone, and ketoconazole combination therapy as an alternative to rescue adrenalectomy for severe ACTH-dependent Cushing's syndrome
    Peter Kamenicky
    Faculte de Medecine Paris Sud, Unité Mixte de Recherche S693, and Institut National de la Santé et de la Recherche Médicale Unité 693, Universite Paris Sud, Le Kremlin Bicêtre F 94276, France
    J Clin Endocrinol Metab 96:2796-804. 2011
    ..Mitotane combined with fast-acting steroidogenesis inhibitors might avoid the need for emergency bilateral adrenalectomy in patients with severe hypercortisolism...
  46. ncbi Identification of ketoconazole as an AhR-Nrf2 activator in cultured human keratinocytes: the basis of its anti-inflammatory effect
    Gaku Tsuji
    Department of Dermatology, Graduate School of Medical Sciences, Kyushu University, Fukuoka, Japan
    J Invest Dermatol 132:59-68. 2012
    b>Ketoconazole (KCZ) has been shown to exhibit anti-inflammatory effects in addition to its inhibitory effects against fungi; however, the underlying molecular mechanism remains poorly understood...
  47. ncbi A randomised, single-blind, single-centre clinical trial to evaluate comparative clinical efficacy of shampoos containing ciclopirox olamine (1.5%) and salicylic acid (3%), or ketoconazole (2%, Nizoral) for the treatment of dandruff/seborrhoeic dermatitis
    R A Squire
    PPD Development, Chelmsford, Essex, UK
    J Dermatolog Treat 13:51-60. 2002
    ..Due to its antimycotic activity, ciclopirox olamine is established as an effective treatment for these scalp conditions. Salicylic acid has keratolytic properties and aids in the removal of scales...
  48. ncbi In vitro susceptibility testing of ciclopirox, terbinafine, ketoconazole and itraconazole against dermatophytes and nondermatophytes, and in vitro evaluation of combination antifungal activity
    A K Gupta
    Division of Dermatology, Department of Medicine, Sunnybrook and Women s College Health Science Center, Sunnybrook Site, and the University of Toronto, Toronto, ON, Canada
    Br J Dermatol 149:296-305. 2003
    ....
  49. ncbi Increased brain uptake of docetaxel and ketoconazole loaded folate-grafted solid lipid nanoparticles
    Vinay Kumar Venishetty
    Department of Pharmaceutical Sciences, Texas Tech University Health Science Center, 1406 S Coulter, Amarillo, TX 79106, USA
    Nanomedicine 9:111-21. 2013
    ..A potential drug-drug interaction exists between docetaxel and ketoconazole because both agents are metabolized hepatically by the cytochrome P-450 system, and ketoconazole can inhibit p-..
  50. ncbi Hydrogel of ketoconazole and PAMAM dendrimers: formulation and antifungal activity
    Katarzyna Winnicka
    Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2c, 15 222 Białystok, Poland
    Molecules 17:4612-24. 2012
    b>Ketoconazole (KET), an imidazole derivative with well-known antifungal properties, is lipophilic and practically insoluble in water, therefore its clinical use has some practical disadvantages...
  51. ncbi Activated pregnenolone X-receptor is a target for ketoconazole and its analogs
    Hongwei Wang
    Albert Einstein Cancer Center, Department of Medicine, Albert Einstein College of Medicine, Bronx, New York 10461, USA
    Clin Cancer Res 13:2488-95. 2007
    ..Because the orphan receptor, pregnenolone X-receptor (PXR), coordinately regulates the expression of paclitaxel metabolizing and transport enzymes, controlling this process could improve therapeutic outcome...
  52. ncbi Ketoconazole and miconazole are antagonists of the human glucocorticoid receptor: consequences on the expression and function of the constitutive androstane receptor and the pregnane X receptor
    Cedric Duret
    INSERM U632, Hepatic Physiopathology, 1919 Route de Mende, 34293 Montpellier, France
    Mol Pharmacol 70:329-39. 2006
    ..In the current study, we investigated the effect of ketoconazole and other azole-derived drugs, miconazole and fluconazole, on the transcriptional activity of the human GR (hGR)..
  53. ncbi Ketoconazole potentiates terfenadine-induced apoptosis in human Hep G2 cells through inhibition of cytochrome p450 3A4 activity
    Ying Jan Wang
    Department of Environmental and Occupational Health, National Cheng Kung University Medical College, Tainan, Taiwan
    J Cell Biochem 87:147-59. 2002
    ..b>Ketoconazole (KT) is a worldwide used oral antifungal agent with a broad spectrum of activity against both superficial and ..
  54. ncbi Sources of variability in ketoconazole inhibition of human cytochrome P450 3A in vitro
    David J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts Medical Center, Boston, MA, USA
    Xenobiotica 40:713-20. 2010
    Despite the extensive use of ketoconazole as an index inhibitor of human cytochrome P450 3A (CYP3A) isoforms in vitro, literature reports of the quantitative inhibitory potency of ketoconazole are highly variable...
  55. ncbi Population-based case-control study of oral ketoconazole treatment for birth outcomes
    Zoltán Kazy
    Foundation for the Community Control of Hereditary Diseases, Budapest, Hungary
    Congenit Anom (Kyoto) 45:5-8. 2005
    The objective of the study presented here was to check the effect of oral ketoconazole treatment on fetal development...
  56. pmc Metal-drug synergy: new ruthenium(II) complexes of ketoconazole are highly active against Leishmania major and Trypanosoma cruzi and nontoxic to human or murine normal cells
    Eva Iniguez
    Department of Biological Sciences, Border Biomedical Research Center, The University of Texas at El Paso, El Paso, TX, 79968, USA
    J Biol Inorg Chem 18:779-90. 2013
    ..search for new metal-based chemotherapeutic agents against leishmaniasis and Chagas disease, six new ruthenium-ketoconazole (KTZ) complexes have been synthesized and characterized, including two octahedral coordination complexes-cis,..
  57. ncbi Phase II trial assessing granulocyte-macrophage-colony stimulating factor, ketoconazole plus mitoxantrone in metastatic castration-resistant prostate cancer progressing after docetaxel treatments
    Robert J Amato
    The University of Texas Health Science Center at Houston, Department of Internal Medicine, Division of Oncology, Houston, Texas 77030, USA
    Cancer Invest 31:177-82. 2013
    ..objective response and safety for the combination of granulocyte macrophage-colony stimulating factor (GM-CSF), ketoconazole, and mitoxantrone in castration-resistant prostate cancer (CRPC) patients who previously failed docetaxel-based ..
  58. ncbi Cyclosporine and ketoconazole for the treatment of perianal fistulas in dogs
    Alison J Patricelli
    Department of Surgical Sciences, School of Veterinary Medicine, University of Wisconsin Madison, 53762, USA
    J Am Vet Med Assoc 220:1009-16. 2002
    To evaluate efficacy and cost of using cyclosporine and ketoconazole for the treatment of perianal fistulas in dogs.
  59. ncbi High-dose ketoconazole in advanced hormone-refractory prostate cancer: endocrinologic and clinical effects
    D L Trump
    University of Wisconsin Clinical Cancer Center, Madison
    J Clin Oncol 7:1093-8. 1989
    High-dose ketoconazole (400 mg orally three times a day) and physiologic replacement doses of glucocorticoids (hydrocortisone, 20 mg 8 AM, 10 mg 4 PM, and 8 PM) were administered to 38 patients with advanced prostatic cancer, refractory ..
  60. pmc Effect of ketoconazole on the pharmacokinetics of axitinib in healthy volunteers
    Yazdi K Pithavala
    Pfizer Oncology, 10555 Science Center Drive, San Diego, CA 92121, USA
    Invest New Drugs 30:273-81. 2012
    ..This study evaluated changes in axitinib plasma pharmacokinetic parameters and assessed safety and tolerability in healthy subjects, following axitinib co-administration with the potent CYP3A inhibitor ketoconazole.
  61. ncbi CYP3A5*1/*3 genotype influences the blood concentration of tacrolimus in response to metabolic inhibition by ketoconazole
    Nirupama Chandel
    Department of Nephrology, Postgraduate Institute of Medical Education and Research, Chandigarh, India
    Pharmacogenet Genomics 19:458-63. 2009
    b>Ketoconazole retards metabolic degradation of tacrolimus through its effect on the cytochrome P-450 enzyme system and allows reduction in treatment costs...
  62. ncbi Steroid synthesis inhibition with ketoconazole and its effect upon the regulation of the hypothalamus-pituitary-adrenal system in healthy humans
    Michael Deuschle
    Central Institute of Mental Health, Mannheim, Germany
    Neuropsychopharmacology 28:379-83. 2003
    ..We studied the effect of treatment with 800 mg ketoconazole (3 weeks) upon the concentrations of basal plasma cortisol in the evening, corticosteroid-binding globulin (CBG)..
  63. ncbi Activity of ketoconazole after taxane-based chemotherapy in castration-resistant prostate cancer
    Mari Nakabayashi
    Lank Center for Genitourinary Oncology, Department of Medical Oncology, Dana Farber Cancer Institute and Harvard Medical School, Boston, MA 02115, USA
    BJU Int 105:1392-6. 2010
    To assess the efficacy of the androgen-synthesis inhibitor ketoconazole as a secondary hormonal therapy in patients with castration-resistant prostate cancer (CRPC) previously treated with chemotherapy, as persistent androgens appear to ..
  64. ncbi Modulation of the cytochrome P450-mediated metabolism of ifosfamide by ketoconazole and rifampin
    T Kerbusch
    Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute, Amsterdam
    Clin Pharmacol Ther 70:132-41. 2001
    ..The aim of this study was to investigate modulation of the CYP-mediated metabolism of ifosfamide with ketoconazole, a potent inhibitor of CYP3A4, and rifampin (INN, rifampicin), an inducer of CYP3A4/CYP2B6.
  65. ncbi Treatment of cutaneous leishmaniasis with ketoconazole cream
    A Z Momeni
    Isfahan University of Medical Sciences, PO Box 81465 1191, Isfahan, Iran
    J Dermatolog Treat 14:26-9. 2003
    ..Many drugs have been suggested for the treatment of CL but most of them used intramuscularly or intravenously. Recently, a ketoconazole tablet has been used for the treatment of CL.
  66. ncbi Rationale for combination ketoconazole/ vitamin D treatment of prostate cancer
    D M Peehl
    Department of Urology, Stanford University School of Medicine, Stanford, California, USA
    Urology 58:123-6. 2001
    ..Adjuvant therapy combined with androgen deprivation may slow or prevent progression. Ketoconazole plus calcitriol therapy is an example of 1 such a combination with a mechanistic basis for synergistic activity...
  67. ncbi Pharmacokinetic modulation of oral etoposide by ketoconazole in patients with advanced cancer
    Wei Peng Yong
    Committee on Clinical Pharmacology and Pharmacogenomics, University of Chicago, 5841 S Maryland Ave, MC2115, Chicago, IL 60637, USA
    Cancer Chemother Pharmacol 60:811-9. 2007
    ..Hence, this study was designed to evaluate if pharmacokinetic modulation of oral etoposide with ketoconazole could lead to a favorable alteration of etoposide pharmacokinetics, and to assess the feasibility and safety of ..
  68. ncbi Ocular pharmacokinetics of topically-applied ketoconazole solution containing hydroxypropyl beta-cyclodextrin to rabbits
    Junjie Zhang
    Pharmaceutic and Pharmacology Department, Henan Eye Institute, Henan Key Laboratory of Keratopathy, Zhengzhou, China
    J Ocul Pharmacol Ther 24:501-6. 2008
    The aim of this study was to develop an aqueous ketoconazole (KET) eye drop in order to increase the corneal permeability and improve ocular bioavailability following topical application.
  69. ncbi NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds
    Joerg Konter
    Institute of Pharmacy, Department of Pharmaceutical Medicinal Chemistry, Friedrich Schiller University Jena, Philosophenweg 14, D 07743 Jena, Germany
    Bioorg Med Chem 16:8294-300. 2008
    Novel hybrid compounds combining the antifungal drug ketoconazole with a diazen-1-ium-1,2-diolate or an organic nitrate moiety and the corresponding NO-donors without ketoconazole were synthesized and their activities against a broad ..
  70. ncbi Ketoconazole: a review of a workhorse antifungal molecule with a focus on new foam and gel formulations
    Noah Scheinfeld
    Department of Dermatology, Columbia University, New York, NY 10019, USA
    Drugs Today (Barc) 44:369-80. 2008
    Topical ketoconazole, an imidazole, has been a mainstay of treatment for fungal infections and seborrheic dermatitis...
  71. ncbi The pharmacokinetics of ketoconazole and its effects on the pharmacokinetics of midazolam and fentanyl in dogs
    B Kukanich
    Department of Anatomy and Physiology, College of Veterinary Medicine, Kansas State University, Manhattan, KS 66506, USA
    J Vet Pharmacol Ther 33:42-9. 2010
    b>Ketoconazole inhibits the Cytochrome P450 3A12 (CYP3A12) metabolizing enzyme as well as the p-glycoprotein efflux pump. The extent and clinical consequence of these effects are poorly understood in dogs...
  72. ncbi Retrospective analysis of the consequences of acid suppressive therapy on ketoconazole efficacy in advanced castration-resistant prostate cancer
    Sidney V Keisner
    Texas Tech University Health Sciences Center, Dallas, USA
    Ann Pharmacother 44:1538-44. 2010
    The area under the curve of a single ketoconazole dose has been shown to decrease significantly when administered with acid suppressive therapy...
  73. ncbi Anti-Candida effects of estragole in combination with ketoconazole or amphotericin B
    Seungwon Shin
    College of Pharmacy, Duksung Women s University, Seoul, Korea
    Phytother Res 18:827-30. 2004
    The anti-Candida effects of estragole combined with amphotericin B or ketoconazole, commonly used antifungal drugs for treatment of candidasis, were evaluated in this study...
  74. pmc Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin
    Joachim Troost
    Boehringer Ingelheim Pharma GmbH and Co KG, Ingelheim, Germany
    Br J Clin Pharmacol 72:247-56. 2011
    ..However, data on potential drug-drug interactions between tamsulosin and inhibitors of CYP2D6 and 3A4 are limited and information on potential pharmacodynamic consequences of such pharmacokinetic interactions is missing...
  75. ncbi Effect of the CYP3A inhibitor ketoconazole on the pharmacokinetics and pharmacodynamics of bortezomib in patients with advanced solid tumors: a prospective, multicenter, open-label, randomized, two-way crossover drug-drug interaction study
    Karthik Venkatakrishnan
    Millennium Pharmaceuticals, Inc, Cambridge, Massachusetts 02139, USA
    Clin Ther 31:2444-58. 2009
    ..The proteasome inhibitor bortezomib undergoes oxidative biotransformation via multiple cytochrome P450 (CYP) enzymes, with CYP3A4 identified as a partial, yet potentially important, contributor based on in vitro drug metabolism studies...
  76. ncbi Ketoconazole, an antifungal agent, protects against adiposity induced by a cafeteria diet
    J Campion
    Department of Physiology and Nutrition, University of Navarra, C Irunlarrea, 31008 Pamplona, Spain
    Horm Metab Res 36:485-91. 2004
    b>Ketoconazole, an anti-glucocorticoid agent, is widely used in humans as an antifungal agent. It inhibits ergosterol synthesis and reduces cortisol levels in the treatment of Cushing's Syndrome...
  77. ncbi Inhibition of UDP-glucuronosyltransferase 2b7-catalyzed morphine glucuronidation by ketoconazole: dual mechanisms involving a novel noncompetitive mode
    Shuso Takeda
    Graduate School of Pharmaceutical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
    Drug Metab Dispos 34:1277-82. 2006
    ..we investigated the effects of P450 inhibitors (cimetidine, sulfaphenazole, erythromycin, nifedipine, and ketoconazole) on the UGT2B7-catalyzed formation of morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G)...
  78. ncbi In vitro antifungal activities of Allium cepa, Allium sativum and ketoconazole against some pathogenic yeasts and dermatophytes
    Masoomeh Shams-Ghahfarokhi
    Department of Mycology, Faculty of Medical Sciences, Tarbiat Modarress University, Tehran 14115 111, Iran
    Fitoterapia 77:321-3. 2006
    ..well as 35 strains of various dermatophyte species and compared with the activity of a known antifungal drug, ketoconazole (KTZ)...
  79. ncbi Use of oral ketoconazole to prevent postoperative erections following penile surgery
    K C Evans
    Urology Service, Madigan Army Medical Center, Tacoma, Washington 98431, USA
    Int J Impot Res 16:346-9. 2004
    Analgesics and topical agents ineffectively inhibit painful erections after penile and urethral surgery. Oral ketoconazole reversibly inhibits testosterone production and has been used empirically at our institution to decrease ..
  80. ncbi Microbiological assay of ketoconazole in shampoo
    Inara Staub
    Programa de Pós Graduação em Ciências Farmacêuticas, UFRGS, Av Ipiranga 2752 Porto Alegre CEP 90610 000, Brasil
    Int J Pharm 292:195-9. 2005
    b>Ketoconazole, an anti-fungal agent, is often incorporated in several pharmaceutical forms and in shampoo formulation it is known to be effective against fungal infection on the scalp...
  81. ncbi Spectroscopic and kinetic studies on the interaction of ketoconazole and povidone drugs with DDQ
    M Pandeeswaran
    Department of Chemistry, Gandhigram Rural University, Gandhigram 624302, India
    Spectrochim Acta A Mol Biomol Spectrosc 69:1082-8. 2008
    The kinetics and mechanism of the interaction between 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) and ketoconazole and povidone drugs has been investigated spectroscopically...
  82. ncbi Efficacy of low-dose ketoconazole in hormone refractory prostate cancer patients at the National Cancer Centre and The Cancer Institute, Singapore
    Lynette S M Ngo
    Department of Medical Oncology, National Cancer Centre, Singapore
    Ann Acad Med Singapore 36:811-4. 2007
    ..b>Ketoconazole, an antimycotic which affects the synthesis of androgens and other steroids, has shown direct cytotoxic effects ..
  83. ncbi The role of ketoconazole in seborrheic dermatitis
    Marcel Borgers
    Barrier Therapeutics NV, Geel, Belgium
    Cutis 80:359-63. 2007
    Although the prominent broad-spectrum activity of ketoconazole was reported in the early 1980s, its effect against Malassezia species was most pronounced; thus, it was developed for the treatment of various skin infections in which a link ..
  84. ncbi Nonlinear stereoselective pharmacokinetics of ketoconazole in rat after administration of racemate
    Dalia A Hamdy
    Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada
    Chirality 21:704-12. 2009
    The stereoselective pharmacokinetics of ketoconazole (KTZ) enantiomers were studied in rat after i.v. and oral administration of (+/-)-KTZ. Sprague-Dawley rats were administered racemic KTZ as 10 mg/kg i.v...
  85. ncbi Inhibition of CYP3A4 expression by ketoconazole is mediated by the disruption of pregnane X receptor, steroid receptor coactivator-1, and hepatocyte nuclear factor 4alpha interaction
    Yun Ping Lim
    Department of Pharmacology, Medical College, National Cheng Kung University, Tainan, Taiwan
    Pharmacogenet Genomics 19:11-24. 2009
    Earlier studies have shown that ketoconazole inhibits CYP3A4 expression through pregnane X receptor (PXR)-mediated transcription and coactivator interaction. The involvement of other nuclear receptors remains to be elucidated...
  86. ncbi Effect of coadministration of ketoconazole, a strong CYP3A4 inhibitor, on pharmacokinetics and tolerability of motesanib diphosphate (AMG 706) in patients with advanced solid tumors
    Patricia LoRusso
    Karmanos Cancer Institute, 4100 John R, 4 HWCRC, Detroit, MI, 48201, USA
    Invest New Drugs 26:455-62. 2008
    ..The purpose of this phase 1b, drug-drug interaction study was to investigate the effect of ketoconazole, a strong inhibitor of the cytochrome P450 3A4 isoenzyme, on the pharmacokinetics and tolerability of motesanib ..
  87. ncbi A new ketoconazole topical gel formulation in seborrhoeic dermatitis: an updated review of the mechanism
    Jan Faergemann
    Sahlgrenska University Hospital, Department of Dermatology, SE 41345 Goteborg, Sweden
    Expert Opin Pharmacother 8:1365-71. 2007
    ..SD responds to the use of antifungal medications such as ketoconazole, suggesting that the inflammation could be linked to the Malassezia spp...
  88. ncbi Antifungal effects of the volatile oils from Allium plants against Trichophyton species and synergism of the oils with ketoconazole
    M S Pyun
    College of Pharmacy, Duksung Women s University, Seoul 132 714, Republic of Korea
    Phytomedicine 13:394-400. 2006
    ..The combined effects of Allium oils with ketoconazole were tested by the checkerboard titer test. Among the tested oils, A. sativum for...
  89. ncbi Impact of nonlinear midazolam pharmacokinetics on the magnitude of the midazolam-ketoconazole interaction in rats
    Ragini Vuppugalla
    Metabolism and Pharmacokinetics, Department of Pharmaceutical Candidate Optimization, Bristol Mye s Squibb Co, P O Box 4000, Princeton, NJ 08543, USA
    Xenobiotica 42:1058-68. 2012
    ..Even for a well-established substrate-inhibitor pair like midazolam-ketoconazole, however, the magnitude of the DDI in rats (e.g. 1...
  90. ncbi Effect of multiple dosing of ketoconazole on pharmacokinetics of midazolam, a cytochrome P-450 3A substrate in beagle dogs
    Masanori Kuroha
    Department of Veterinary Medicine, Tokyo University of Agriculture and Technology, 3 5 8 Saiwai cho, Fuchu, Tokyo 183 0054, Japan
    Drug Metab Dispos 30:63-8. 2002
    To evaluate effects of multiple dosing of ketoconazole (KTZ) on hepatic CYP3A, the pharmacokinetics of intravenous midazolam (MDZ, 0.5 mg/kg) before and during multiple dosing of KTZ were investigated in beagle dogs...
  91. ncbi Ketoconazole-associated preferential increase in dopamine D2 receptor occupancy in striatum compared to pituitary in vivo: role for drug transporters?
    Christopher Reist
    VA Long Beach Healthcare System, Long Beach, CA, USA
    J Clin Psychopharmacol 32:110-3. 2012
    ..We report here that coadministration of the P-gp and BCRP inhibitor ketoconazole with risperidone may preferentially increase D2 receptor occupancy in the striatum compared to pituitary...
  92. ncbi Fatal liver failure due to ketoconazole treatment of a girl with Cushing's syndrome
    E Zollner
    Department of Paediatrics, University of Cape Town, South Africa
    J Pediatr Endocrinol Metab 14:335-8. 2001
    A patient is reported who developed fatal liver failure on ketoconazole treatment for Cushing's syndrome...
  93. ncbi Assessment of the drug interaction risk for remogliflozin etabonate, a sodium-dependent glucose cotransporter-2 inhibitor: evidence from in vitro, human mass balance, and ketoconazole interaction studies
    James F Sigafoos
    Departments of Drug Metabolism and Pharmacokinetics, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
    Drug Metab Dispos 40:2090-101. 2012
    ..A ketoconazole clinical drug interaction study, along with the human mass balance findings, confirmed that CYP3A4 contributes ..
  94. ncbi Differential effects of ketoconazole and primaquine on the pharmacokinetics and tissue distribution of imatinib in mice
    Gian Wan Soo
    Department of Pharmaceutical Technology, International Medical University, Kuala Lumpur, Malaysia
    Anticancer Drugs 21:695-703. 2010
    ..interaction with primaquine, which also binds to alpha-1-acid glycoprotein, and its metabolic interaction with ketoconazole, which is a CYP3A4 inhibitor, on its pharmacokinetics and biodistribution...
  95. ncbi Systemic ketoconazole is an effective treatment of atopic dermatitis with IgE-mediated hypersensitivity to yeasts
    P Lintu
    Department of Dermatology, Turku Allergy Research Unit, MediCity Research Laboratory, University of Turku, Turku, Finland
    Allergy 56:512-7. 2001
    ..Two studies have shown the efficacy of ketoconazole in the treatment of this type of AD, in contrast to results of topical treatment...
  96. ncbi In vitro-in vivo extrapolation predicts drug-drug interactions arising from inhibition of codeine glucuronidation by dextropropoxyphene, fluconazole, ketoconazole, and methadone in humans
    Pritsana Raungrut
    Department of Clinical Pharmacology, Flinders University School of Medicine, Adelaide, Australia
    J Pharmacol Exp Ther 334:609-18. 2010
    ..Inhibition screening identified potential interactions with dextropropoxyphene, fluconazole, ketoconazole, and methadone. Inhibitor constant values generated for dextropropoxyphene (3...
  97. ncbi Ketoconazole-induced JNK phosphorylation and subsequent cell death via apoptosis in human osteosarcoma cells
    Ko Long Lin
    Department of Rehabilitation, Kaohsiung Veterans General Hospital, 813 Kaohsiung, Taiwan
    Toxicol In Vitro 23:1268-76. 2009
    This study examined the effect of ketoconazole on viability, apoptosis, mitogen-activated protein kinases (MAPKs) and Ca(2+) levels in MG63 osteosarcoma cells...
  98. ncbi Ketoconazole: a thromboxane synthetase and 5-lipoxygenase inhibitor with antimetastatic activity in B16-F10 melanoma
    P A Nardone
    Department of Internal Medicine, University of Massachusetts Medical School, Worcester
    J Surg Res 44:425-9. 1988
    ..The purpose of this study was to determine the antimetastatic potential of ketoconazole, a thromboxane synthetase and 5-lipoxygenase inhibitor...
  99. pmc The cytochrome P450 inhibitor, ketoconazole, inhibits oxidized linoleic acid metabolite-mediated peripheral inflammatory pain
    Shivani Ruparel
    Department of Endodontics, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, USA
    Mol Pain 8:73. 2012
    ....
  100. ncbi Anti-Aspergillus activities of plant essential oils and their combination effects with ketoconazole or amphotericin B
    Seungwon Shin
    College of Pharmacy, Duksung Women s University, Seoul 132 714, Korea
    Arch Pharm Res 26:389-93. 2003
    ..graveolens on the antifungal activity of amphotericin B and ketoconazole were examined using a checkerboard microtiter assay against both Aspergillus fungi...
  101. pmc A controlled study to determine the efficacy of Loxostylis alata (Anacardiaceae) in the treatment of aspergillus in a chicken (Gallus domesticus) model in comparison to ketoconazole
    Mohammed M Suleiman
    Phytomedicine Programme, Department of Paraclinical Sciences, Faculty of Veterinary Science, University of Pretoria, Pretoria, South Africa
    BMC Vet Res 8:210. 2012
    ..07 mg/ml. For this study crude, a crude acetone extract of L. alata leaves was evaluated for its acute toxicity in a healthy chicken model and for efficacy in an infectious model of aspergillosis (A. fumigatus)...

Research Grants63

  1. Triazole hypersensitivity in Candida albicans
    Neeraj Chauhan; Fiscal Year: 2009
    ..the ssk1 mutant retains the wild type levels of sensitivity to other antifungals such as miconazole and ketoconazole (imidazoles), amphotericin B, caspofungin, 5-FC, and a variety of other inhibitors such as Congo red, ..
  2. Mechanisms of Drug Induced Phospholipidosis
    JAMES ALAN SHAYMAN; Fiscal Year: 2013
    ..include, but are not limited to, azithromycin, fluoxetine, amiodarone, chloroquine, imipramine, and ketoconazole. Ascertaining the significance of this complication has been problematic for clinicians, as well as scientists ..
  3. Characterization of a Novel Selective Cytochrome P450 3A5 Substrate
    MICHAEL DARIN CAMERON; Fiscal Year: 2013
    ..Some drugs such as ketoconazole have been shown to inhibit the activity of individual P450 enzymes;while other drugs such as rifampicin or ..
  4. AGE-RELATED GASTRIC CHANGES AND DRUG ABSORPTION
    Aryeh Hurwitz; Fiscal Year: 1993
    ..the second year, studies will begin of gastrointestinal absorption of the anti-infective agents, enoxacin and ketoconazole. The solubility of both drugs is markedly reduced at pH above 5 and their absorption is depressed by ..
  5. DRUG METABOLISM BY INTESTINAL FLAVIN MONOOXYGENASES
    ROSITA PROTEAU; Fiscal Year: 2001
    ..inhibitory or stimulatory effects of flavonoids on the metabolism of methimazole, cimetidine, and N-deacetyl ketoconazole will be evaluated using cDNA-expressed human FMOs...
  6. Chemical Modulation of Orphan Nuclear Receptor Function
    Sridhar Mani; Fiscal Year: 2013
    ..Towards this end, we have identified and characterized two novel PXR antagonists, ketoconazole and coumestrol, that specifically disrupt the function of activated (ligand-bound) PXR...
  7. YEAST ERGOSTEROL PATHWAY--NEW ANTIFUNGAL TARGET SITES
    Martin Bard; Fiscal Year: 1999
    ..classes, the polyenes (amphotericin B) target plasma membrane-bound sterols and the new classes of azoles (ketoconazole, fluconazole, and itraconazole) target the cytochrome P450-mediated step, lanosterol C-14 demethylation...
  8. REDUCED DRUG INTERACTIONS OF AZOLE ANTIFUNGAL DRUGS
    Joseph Gal; Fiscal Year: 2003
    The incidence of serious fungal infections has increased considerably in recent decades. The "azoles" ketoconazole and itraconazole are important and widely-used oral antifungal agents, but the use of these drugs is limited by adverse ..
  9. Evaluation of CYP24 as a Target for Enhancing Vitamin D*
    Donald Trump; Fiscal Year: 2006
    ..We have shown that ketoconazole, an inhibitor of CYP24, enhances the anti-tumor effects of calcitriol and decreases CYP24 activity in ..
  10. Chronic Nicotine's Activation of the HPA Axis
    Theodore Friedman; Fiscal Year: 2005
    ..The use of agents which modify the stress response such as glucocorticoid synthesis inhibitors (ketoconazole, aminoglutethimide or metyrapone) or antagonists (RU-486), CRH antagonists, such as antalarmin, or agents which ..
  11. GLUCOCORTICOIDS & VITAMIN D: ROLE IN ANTI-TUMOR EFFECTS
    Candace Johnson; Fiscal Year: 2009
    ..b>Ketoconazole, an inhibitor of CYP24, the enzyme responsible of catabolism of calcitriol, can synergize with calcitriol and ..
  12. PHARMACOTHERAPY OF CUE INDUCED COCAINE CRAVING
    S Berger; Fiscal Year: 2000
    ..The steroid synthesis inhibitor ketoconazole will be used to inhibit cue- induces increases in cortisol (component 1, Cue Reactivity) If medications can be ..
  13. Targeting Androgen -IGF Interactions in Prostate Cancer
    Charles Ryan; Fiscal Year: 2009
    ..A widely utilized approach to reducing adrenal androgen production is the use of ketoconazole, an inhibitor of adrenal steroid biosynthesis...
  14. Human Metabolism of Anti-Abuse Medications
    David Moody; Fiscal Year: 2005
    ..The proposal funded during the last period (R01 DA 10100-02) tested the hypothesis that the 3A4 inhibitor, ketoconazole, would inhibit the metabolism of LAAM to its more active metabolites, norLAAM and dinorLAAM, and thereby ..
  15. REGULATION OF ENZYMES IN MEVALONATE SYNTHESIS
    HARRY RUDNEY; Fiscal Year: 1991
    ..We have found that U18666A ketoconazole and progesterone can inhibit the formation of regulatory oxysterols and allow accumulation of precursors of ..
  16. ENDOGENOUS FUNGAL ENDOPHTHALMITIS
    Dan Jones; Fiscal Year: 1980
    ..Intravenous amphotericin B, intravenous amphotericin B methyl ester, and oral ketoconazole reduce the severity of C...
  17. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2006
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  18. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2003
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  19. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2005
    ....
  20. MDR1 and Related Proteins during HIV PI Exposure
    David Greenblatt; Fiscal Year: 2005
    ..The findings will be of importance in understanding lipid disorders related to PIs as well as the kinetics of drugs used to treat HIV and related disorders. ..
  21. ANTIRETROVIRAL THERAPIES AND SUBSTANCE ABUSE
    David Greenblatt; Fiscal Year: 2002
    ..The in vitro model, if validated, has the potential to provide clinically important information on interactions involving HIV treatments and abusable drugs, at relatively low cost and with no human drug exposure. ..
  22. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  23. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
    ....
  24. Sterol Biosynthesis in Trypanosomatid Parasites
    Frederick Buckner; Fiscal Year: 2004
    ..The drugs discovered in this research program will hopefully provide better future treatment for patients with these devastating diseases. ..
  25. Ensemble Disruption of the GnRH-LH-Testosterone Axis
    Johannes Veldhuis; Fiscal Year: 2007
    ..Expected corollary outcomes are enhanced diagnosis, assessment and management of more subtle pathophysiology of the male gonadal axis in puberty and adulthood. ..
  26. Mechanistic bases for age-related androgen deficiency
    Johannes Veldhuis; Fiscal Year: 2007
    ..Knowing why testosterone falls should help foster new and safer ways to prevent the problem. [unreadable] [unreadable] [unreadable]..
  27. Analytical Reconstruction of Feedback Signaling in Aging Men
    Johannes Veldhuis; Fiscal Year: 2008
    ..The present proposal develops a general biomathematical framework for dissecting otherwise observed pathways that control hormone output in aging, stress and disease. [unreadable] [unreadable] [unreadable]..
  28. REGULATION OF CYTOCHROME P4503A ACTIVITY IN THE ELDERLY
    Lisa von Moltke; Fiscal Year: 2004
    ....
  29. ACTIONS OF ESTROGEN IN MATURING GRAAFIAN FOLLICLES
    Johannes Veldhuis; Fiscal Year: 2005
    ..Understanding such fundamental interactions is important to the rational design of alternative strategies to interrupt normal and rescue impaired steroidogenesis in the maturing Graafian follicle and corpus luteum. ..
  30. ENSEMBLE MODEL OF STRESS ACTH-ADRENAL AXIS
    Johannes Veldhuis; Fiscal Year: 2005
    ....
  31. Novel Active Repressor Model of Human LDL-Receptor Regulation
    Johannes Veldhuis; Fiscal Year: 2008
    ..This would represent a new treatment approach for patients with atherosclerotic disease. [unreadable] [unreadable] [unreadable] [unreadable]..
  32. THE AGING GH AXIS IN POSTMENOPAUSAL WOMEN
    Johannes Veldhuis; Fiscal Year: 2005
    ..An enhanced knowledge base should aid ultimately in formulating more innovative preventive and interventional strategies to limit hyposomatotropism in older and/or estrogen-deficient humans. ..
  33. Functional Infrared Imaging Predicts Radiation Mucositis
    Ezra Cohen; Fiscal Year: 2008
    ..Such a tool would have wide applicability in this patient population and would have tremendous impact on their treatment. [unreadable] [unreadable] [unreadable]..
  34. Neurochemistry of Cocaine Reinforcement
    NICHOLAS GOEDERS; Fiscal Year: 2002
    ..These results will also provide evidence of the role that is played by steroid hormones in shaping the functional activity of the brain. ..
  35. Role of CRH in skin physiology and pathology
    Andrzej Slominski; Fiscal Year: 2004
    ..g., melanocytes and keratinocytes, and test the role of CRH/CRH-R1 axis in the regulation of human hair growth. ..
  36. Pharmacogenetics of Methadone
    C Devane; Fiscal Year: 2003
    ..This study will form the basis for subsequent studies which should provide a more rational basis for dosing of methadone in pregnant addicts. ..
  37. Genetics of Opioid Dependence in a Hmong (Thai) Isolate
    Robert Malison; Fiscal Year: 2007
    ..Such studies, we believe, afford significant, perhaps uniquely powerful, advantages for identifying susceptibility loci for OD. [unreadable] [unreadable] [unreadable] [unreadable]..
  38. SPECT IMAGING OF DOPAMINE FUNCTION IN DAYTOP SUBJECTS
    Robert Malison; Fiscal Year: 2001
    ..abstract_text> ..
  39. Molecular Targets of Novel Antifungal Compounds
    Ameeta Agarwal; Fiscal Year: 2008
    ..This work will provide a starting point in the development of new antifungal therapies. [unreadable] [unreadable] [unreadable]..
  40. Restoration of Muscle Following Hip Surgery
    Arny A Ferrando; Fiscal Year: 2010
    ..The amelioration of hypercortisolemia after surgery will be accomplished with a common antifungal agent, ketoconazole, in order to investigate the resultant affects on muscle protein breakdown...
  41. Bayesian Tools for PBPK Models in Drug Interaction Research
    Lang Li; Fiscal Year: 2009
    ..Hence, a CYP3A specific inhibitor-substrate combination, ketoconazole-midazolam, is chosen as a starting example...
  42. Chondrocyte S100/Calgranulins and RAGE in Osteoarthritis
    Robert Terkeltaub; Fiscal Year: 2009
    ..Completion of the work will reveal new potential targets for therapeutic intervention in OA by disconnecting inflammation from deleterious alteration of chondrocyte differentiation and function. ..
  43. Role for the HPA Axis in Methamphetamine Reinforcement
    NICHOLAS GOEDERS; Fiscal Year: 2005
    ..abstract_text> ..
  44. TGF-BETA, CHLORIDE CHANNELS AND APOPTOSIS OF AIRWAY EPITHELIAL CELLS
    Devendra K Agrawal; Fiscal Year: 2010
    ..Such investigations would provide unique insights to the pathophysiologic process of chronic asthma and the means to prevent or reverse the disease. ..
  45. ANESTHETIC RENAL METABOLISM--MECHANISMS AND CONSEQUENCES
    Evan Kharasch; Fiscal Year: 2002
    ..More broadly, resulting biochemical and clinical insights will be applicable to the numerous other nephrotoxic haloalkenes that are ubiquitous environmental contaminants. ..
  46. Vulnerability to Drug Abuse and Treatment Efficacy: Animal Models
    Marilyn E Carroll; Fiscal Year: 2010
    ..The proposed research will show how enhanced drug-seeking behavior in vulnerable phenotypes can be reduced at the most critical, vulnerable phases of drug abuse through behavioral and pharmacological interventions. ..
  47. Structure/Function Studies on Flavoproteins
    Irina Sevrioukova; Fiscal Year: 2007
    ..unreadable] [unreadable]..
  48. ENVIRONMENTAL INFLUENCES ON COCAINE SELF-ADMINISTRATION
    NICHOLAS GOEDERS; Fiscal Year: 2007
    ..The experiments described in this revised application were designed with these stipulations in mind, taking into consideration the recommendations of the reviewers of the previous submission. ..
  49. TESTOSTERONE EFFECTS ON MUSCLE IN BURN INJURY
    Arny Ferrando; Fiscal Year: 2004
    ..In addition, these studies will investigate the safety and efficacy of inexpensive agents in ameliorating muscle loss after burn injury. ..
  50. Enhancing the Safety of Research Participants
    Donald Trump; Fiscal Year: 2003
    ..abstract_text> ..
  51. HIPPOCAMPAL FUNCTION DURING CORTICOSTEROID THERAPY
    E Sherwood Brown; Fiscal Year: 2004
    ..Through this award, the Pl will extend his previous research experience by adding new skills and knowledge which will be used for investigations at the interface of neuroscience and clinical research. ..
  52. PTHRP 1 to 173 IN CHONDROCYTES
    Robert Terkeltaub; Fiscal Year: 2005
    ..Completion of these studies will indicate not only how PTHrP 1-173 can modulate OA, but also how functional properties of the PTHrP 1-173 C-terminal 140-173 domain can be harnessed to promote cartilage repair. ..
  53. Enzyme Targets-Sterol Synthesis-Opportunistic Pathogens
    WILLIAM NES; Fiscal Year: 2004
    ..The results from these studies will facilitate the design of therapeutic strategies aimed to provide species-specific discrimination of inhibition in the ergosterol biosynthetic pathway. ..
  54. Orthogonal Strategies for Specific Knockout Production
    CY STEIN; Fiscal Year: 2005
    ..Finally, in Specific Aim 4, we will evaluate the molecular consequences of the down regulation of bcl-2 and bcl-xL by employing the 12,000 gene-containing Affymetrix oligonucleotide microarray technology. ..
  55. STRESS AND THE NEUROBIOLOGY OF DRUG AND ALCOHOL DEPENDE
    NICHOLAS GOEDERS; Fiscal Year: 2004
    ..The primary goal of this Training Program is to provide students and young scientists with comprehensive guidance in stress and drug abuse research. ..
  56. Pharmacotherapy for opioid and cocaine dependence
    Bruce Rounsaville; Fiscal Year: 2005
    ..4. To examine depression as a predictor of response. 5. To examine three month follow-up status after completing the treatment trial for continuation in treatment, abstinence from illicit drugs, and depressive symptoms. ..
  57. MOLECULAR STUDIES OF GENE TARGETED OLIGONUCLEOTIDES
    CY STEIN; Fiscal Year: 2002
    ..Finally, in Specific Aim 3, we will amplify the delivery of alt-OMPs and chi-OMPs to cells by condensing them with a novel delivery agent, tetra (N-methylpyridyl) porphine. ..
  58. Cocaine, Disulfiram & DBH: A Pharmacomechanistic Study
    Robert Malison; Fiscal Year: 2004
    ..abstract_text> ..
  59. ADVANCED TRAINING IN SPECT/PET NEURORECEPTOR IMAGING
    Robert Malison; Fiscal Year: 2003
    ..abstract_text> ..
  60. Naltrexone for Bipolar Disorder and Alcohol Dependence
    E Sherwood Brown; Fiscal Year: 2006
    ..Alcohol use is the primary outcome, and alcohol craving is the secondary outcome. Manic and depressive symptom severity and the relationship between changes in alcohol use and changes in mood will be expIored. ..
  61. Screen for Mycobacterium Tuberculosis (RMI)
    E White; Fiscal Year: 2005
    ..tuberculosis. 3) To study the effect of these novel inhibitors on the pantothenate pathway in M. smegmatis. 4) To co-crystallize these compounds with pantothenate synthetase to study their mode of binding ..
  62. Mechanism of Action of G3139
    CY STEIN; Fiscal Year: 2007
    ..unreadable] [unreadable] [unreadable]..
  63. Herb Drug Interactions
    Gary Henderson; Fiscal Year: 2004
    ..abstract_text> ..