ketoconazole

Summary

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

Top Publications

  1. Troost J, Tatami S, Tsuda Y, Mattheus M, Mehlburger L, Wein M, et al. Effects of strong CYP2D6 and 3A4 inhibitors, paroxetine and ketoconazole, on the pharmacokinetics and cardiovascular safety of tamsulosin. Br J Clin Pharmacol. 2011;72:247-56 pubmed publisher
    ..To determine the effect of the strong CYP2D6 inhibitor paroxetine and strong CYP3A4 inhibitor ketoconazole on the pharmacokinetics and safety (orthostatic challenge) of tamsulosin...
  2. Keizman D, Huang P, Carducci M, Eisenberger M. Contemporary experience with ketoconazole in patients with metastatic castration-resistant prostate cancer: clinical factors associated with PSA response and disease progression. Prostate. 2012;72:461-7 pubmed publisher
    ..Compounds targeting CYP-17 hydroxylase and lyase, as ketoconazole and abiraterone, block adrenal/intratumoral androgen biosynthesis, and are used as sequential endocrine ..
  3. Patel M, Patel R, Parikh J, Solanki A, Patel B. Investigating effect of microemulsion components: In vitro permeation of ketoconazole. Pharm Dev Technol. 2011;16:250-8 pubmed publisher
    ..to evaluate the effect of oil, surfactant/co-surfactant mixing ratios and water on the in vitro permeation of ketoconazole (KTZ) applied in O/W microemulsion vehicle through intact rat skin...
  4. Greenblatt D, Zhao Y, Venkatakrishnan K, Duan S, Harmatz J, Parent S, et al. Mechanism of cytochrome P450-3A inhibition by ketoconazole. J Pharm Pharmacol. 2011;63:214-21 pubmed publisher
    b>Ketoconazole is extensively used as an index inhibitor of cytochrome P450-3A (CYP3A) activity in vitro and in vivo, but the mechanism of ketoconazole inhibition of CYP3A still is not clearly established...
  5. Reist C, Wu J, Lilja Y, Mukherjee J, Gripeos D, CONSTANTINESCU C, et al. Ketoconazole-associated preferential increase in dopamine D2 receptor occupancy in striatum compared to pituitary in vivo: role for drug transporters?. J Clin Psychopharmacol. 2012;32:110-3 pubmed publisher
    ..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...
  6. el Sayed M, Anwar A. Intralesional sodium stibogluconate alone or its combination with either intramuscular sodium stibogluconate or oral ketoconazole in the treatment of localized cutaneous leishmaniasis: a comparative study. J Eur Acad Dermatol Venereol. 2010;24:335-40 pubmed publisher
    ..The aim of the present study was to investigate if the combination of intramuscular (IM) SSG or oral ketoconazole with intralesional (IL) SSG would be more effective than the intralesional SSG given alone in the treatment of ..
  7. Ryan C, Smith M, Fong L, Rosenberg J, Kantoff P, Raynaud F, et al. 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. J Clin Oncol. 2010;28:1481-8 pubmed publisher
    ..effects on steroidogenesis and prostate-specific antigen (PSA) levels in men with CPRC with or without prior ketoconazole therapy. Thirty-three men with chemotherapy-naïve progressive CRPC were enrolled...
  8. Kukanich B, Hubin M. The pharmacokinetics of ketoconazole and its effects on the pharmacokinetics of midazolam and fentanyl in dogs. J Vet Pharmacol Ther. 2010;33:42-9 pubmed publisher
    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...
  9. Kim J, Yi S, Kim T, Lim K, Yoon S, Cho J, et al. Increased systemic exposure of fimasartan, an angiotensin II receptor antagonist, by ketoconazole and rifampicin. J Clin Pharmacol. 2013;53:75-81 pubmed publisher
    The authors studied the effects of ketoconazole and rifampicin on the pharmacokinetics of a single dose of fimasartan (BR-A-657), a newly developed angiotensin II receptor antagonist for the treatment of hypertension, in 22 healthy ..

More Information

Publications62

  1. Yan Z, Lu G, Wu D, Ye Q, Xie Z. Interaction of 17?-estradiol and ketoconazole on endocrine function in goldfish (Carassius auratus). Aquat Toxicol. 2013;132-133:19-25 pubmed publisher
    ..The aim of the present study was to evaluate the interactions of two classes of EDCs, 17?-estradiol (E2) and ketoconazole (KTC), on endocrine function in male goldfish (Carassius auratus), including vitellogenesis, metabolic ..
  2. Abbas R, Hug B, Leister C, Burns J, Sonnichsen D. Effect of ketoconazole on the pharmacokinetics of oral bosutinib in healthy subjects. J Clin Pharmacol. 2011;51:1721-7 pubmed publisher
    ..The effect of coadministration of ketoconazole on the pharmacokinetic (PK) profile of bosutinib was evaluated in an open-label, randomized, 2-period, ..
  3. Paul A, Mansfield C, Thompson M. Presumptive Nocardia spp. infection in a dog treated with cyclosporin and ketoconazole. N Z Vet J. 2010;58:265-8 pubmed publisher
    A dog that had received 8 months of cyclosporin and ketoconazole therapy for treatment of atopic dermatitis subsequently developed severe neurological disease, that failed to respond to treatment with trimethoprim-sulphadiazine and ..
  4. Peer A, Gottfried M, Sinibaldi V, Carducci M, Eisenberger M, Sella A, et al. Comparison of abiraterone acetate versus ketoconazole in patients with metastatic castration resistant prostate cancer refractory to docetaxel. Prostate. 2014;74:433-40 pubmed publisher
    ..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...
  5. Womble P, VanVeldhuizen P, Nisbet A, Reed G, Thrasher J, Holzbeierlein J. A phase II clinical trial of neoadjuvant ketoconazole and docetaxel chemotherapy before radical prostatectomy in high risk patients. J Urol. 2011;186:882-7 pubmed publisher
    ..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...
  6. Gupta A, Unadkat J, Mao Q. Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP). J Pharm Sci. 2007;96:3226-35 pubmed
    ..The goal of this study was to investigate the interactions of azole antifungal agents, ketoconazole, itraconazole, fluconazole, and voriconazole, with BCRP...
  7. Kamenicky P, Droumaguet C, Salenave S, Blanchard A, Jublanc C, Gautier J, et al. Mitotane, metyrapone, and ketoconazole combination therapy as an alternative to rescue adrenalectomy for severe ACTH-dependent Cushing's syndrome. J Clin Endocrinol Metab. 2011;96:2796-804 pubmed publisher
    ..Our objective was to assess the efficacy and safety of combination therapy with mitotane, metyrapone, and ketoconazole in severe ACTH-dependent Cushing's syndrome...
  8. Figg W, Woo S, Zhu W, Chen X, Ajiboye A, Steinberg S, et al. A phase I clinical study of high dose ketoconazole plus weekly docetaxel for metastatic castration resistant prostate cancer. J Urol. 2010;183:2219-26 pubmed publisher
    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 ..
  9. Suleiman M, Duncan N, Eloff J, Naidoo V. 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. BMC Vet Res. 2012;8:210 pubmed publisher
    ..The extract was as effective as the positive control ketoconazole dosed at 60 mg/kg. The results indicate that a crude extract of L...
  10. Atsmon J, Dingemanse J, Shaikevich D, Volokhov I, Sidharta P. Investigation of the effects of ketoconazole on the pharmacokinetics of macitentan, a novel dual endothelin receptor antagonist, in healthy subjects. Clin Pharmacokinet. 2013;52:685-92 pubmed publisher
    ..This study aimed to investigate the magnitude of a possible effect of a potent CYP3A4 inhibitor, ketoconazole, on the pharmacokinetics of macitentan...
  11. Castinetti F, Guignat L, Giraud P, Muller M, Kamenicky P, Drui D, et al. Ketoconazole in Cushing's disease: is it worth a try?. J Clin Endocrinol Metab. 2014;99:1623-30 pubmed publisher
    The use of ketoconazole has been recently questioned after warnings from the European Medicine Agencies and the Food and Drug Administration due to potential hepatotoxicity...
  12. Tanaka C, Yin O, Smith T, Sethuraman V, Grouss K, Galitz L, et al. Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants. J Clin Pharmacol. 2011;51:75-83 pubmed publisher
    ..conducted in healthy volunteers prior to and following treatment with a strong inducer (rifampin) or inhibitor (ketoconazole)...
  13. Vilar L, Naves L, Azevedo M, Arruda M, Arahata C, Moura e Silva L, et al. Effectiveness of cabergoline in monotherapy and combined with ketoconazole in the management of Cushing's disease. Pituitary. 2010;13:123-9 pubmed publisher
    ..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...
  14. Taplin M, Regan M, Ko Y, Bubley G, Duggan S, Werner L, et al. Phase II study of androgen synthesis inhibition with ketoconazole, hydrocortisone, and dutasteride in asymptomatic castration-resistant prostate cancer. Clin Cancer Res. 2009;15:7099-105 pubmed publisher
    ..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)...
  15. Sartor O, Nakabayashi M, Taplin M, Ross R, Kantoff P, Balk S, et al. Activity of dutasteride plus ketoconazole in castration-refractory prostate cancer after progression on ketoconazole alone. Clin Genitourin Cancer. 2009;7:E90-2 pubmed publisher
    b>Ketoconazole is a commonly used secondary hormonal therapy in castration-refractory prostate cancer (CRPC), but disease progression inevitably occurs...
  16. Fuchs I, Hafner Blumenstiel V, Markert C, Burhenne J, Weiss J, Haefeli W, et al. Effect of the CYP3A inhibitor ketoconazole on the PXR-mediated induction of CYP3A activity. Eur J Clin Pharmacol. 2013;69:507-13 pubmed publisher
    The aim of this clinical study was to investigate a previously proposed mechanism of ketoconazole-mediated inhibition of cytochrome P450 3A (CYP3A) induction. A two-phase, randomized, cross-over, open, mono-centre trial was carried out...
  17. Vuppugalla R, Zhang Y, Chang S, Rodrigues A, Marathe P. Impact of nonlinear midazolam pharmacokinetics on the magnitude of the midazolam-ketoconazole interaction in rats. Xenobiotica. 2012;42:1058-68 pubmed publisher
    ..Even for a well-established substrate-inhibitor pair like midazolam-ketoconazole, however, the magnitude of the DDI in rats (e.g. 1...
  18. Saka B, Kombate K, Mouhari Toure A, Akakpo S, Tchangaï B, Amegbor K, et al. [Probable basidiobolomycosis in a Togolese rural young successfully treated with ketoconazole]. Bull Soc Pathol Exot. 2010;103:293-5 pubmed publisher
    ..We report a case of basidiobolomycosis successfully treated with ketoconazole. It was a 9-year-old boy of rural origin in whom the diagnosis of basidiobolomycosis was suspected due to a ..
  19. Amber K, Aijaz A, Immaculata X, Luqman K, Nikhat M. Anticandidal effect of Ocimum sanctum essential oil and its synergy with fluconazole and ketoconazole. Phytomedicine. 2010;17:921-5 pubmed publisher
    ..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 ..
  20. Iniguez E, Sanchez A, Vasquez M, Martinez A, Olivas J, Sattler A, et al. 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. J Biol Inorg Chem. 2013;18:779-90 pubmed publisher
    ..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,..
  21. Ruparel S, Green D, Chen P, Hargreaves K. The cytochrome P450 inhibitor, ketoconazole, inhibits oxidized linoleic acid metabolite-mediated peripheral inflammatory pain. Mol Pain. 2012;8:73 pubmed publisher
    ..To determine the role of CYP enzymes in mediating OLAM effects, we used a broad spectrum CYP inhibitor, ketoconazole. Pretreatment with ketoconazole inhibited the release of TRPV1 agonists in lipid extracts from inflamed skin ..
  22. Johnson F, Agrawal S, Burris H, Rosen L, Dhillon N, Hong D, et al. Phase 1 pharmacokinetic and drug-interaction study of dasatinib in patients with advanced solid tumors. Cancer. 2010;116:1582-91 pubmed publisher
    ..term and sequential and was designed to determine whether the coadministration of the potent CYP3A4 inhibitor ketoconazole had an effect on the pharmacokinetics of dasatinib...
  23. Tyl B, Kabbaj M, Azzam S, Sologuren A, Valiente R, Reinbolt E, et al. 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. J Clin Pharmacol. 2012;52:893-903 pubmed publisher
    ..and supratherapeutic doses (20 mg and 100 mg once daily, respectively), and bilastine 20 mg administered with ketoconazole 400 mg...
  24. Soo G, Law J, Kan E, Tan S, Lim W, Chay G, et al. Differential effects of ketoconazole and primaquine on the pharmacokinetics and tissue distribution of imatinib in mice. Anticancer Drugs. 2010;21:695-703 pubmed
    ..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...
  25. Kaeser B, Zandt H, Bour F, Zwanziger E, Schmitt C, Zhang X. Drug-drug interaction study of ketoconazole and ritonavir-boosted saquinavir. Antimicrob Agents Chemother. 2009;53:609-14 pubmed publisher
    ..Saquinavir is coadministered with ritonavir, a strong CYP3A4 inhibitor, to boost its exposure. Ketoconazole is a potent CYP3A inhibitor...
  26. Urban V, Seo R, Giannini M, Arrais C. Superficial distribution and identification of antifungal/antimicrobial agents on a modified tissue conditioner by SEM-EDS microanalysis: a preliminary study. J Prosthodont. 2009;18:603-10 pubmed publisher
    ..The addition of miconazole was at 125 mg (G3) and 250 mg (G4), and ketoconazole was at 100 mg (G5) and 200 mg (G6)...
  27. Shin S, Lim S. Antifungal effects of herbal essential oils alone and in combination with ketoconazole against Trichophyton spp. J Appl Microbiol. 2004;97:1289-96 pubmed
    ..the effects of Pelargonium graveolens oil and its main components citronellol and geraniol combined with ketoconazole against Trichophyton spp. Growth inhibition of six Trichophyton spp...
  28. Seidegard J, Nyberg L, Borgå O. Presystemic elimination of budesonide in man when administered locally at different levels in the gut, with and without local inhibition by ketoconazole. Eur J Pharm Sci. 2008;35:264-70 pubmed publisher
    ..was installed at each location by intubation, with or without immediate prior local administration of 16mg ketoconazole. Simultaneously, deuterium-labelled budesonide (0.2mg) was administered intravenously...
  29. Deuschle M, Lecei O, Stalla G, Landgraf R, Hamann B, Lederbogen F, et al. Steroid synthesis inhibition with ketoconazole and its effect upon the regulation of the hypothalamus-pituitary-adrenal system in healthy humans. Neuropsychopharmacology. 2003;28:379-83 pubmed
    ..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)..
  30. Tzanakakis G, Krambovitis E, Tsatsakis A, Vezeridis M. The preventive effect of ketoconazole on experimental metastasis from a human pancreatic carcinoma may be related to its effect on prostaglandin synthesis. Int J Gastrointest Cancer. 2002;32:23-30 pubmed
    ..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 ..
  31. Zhang X, Hecker M, Tompsett A, Park J, Jones P, Newsted J, et al. Responses of the medaka HPG axis PCR array and reproduction to prochloraz and ketoconazole. Environ Sci Technol. 2008;42:6762-9 pubmed
    Effects of two model imidazole-type fungicides, prochloraz (PCZ) and ketoconazole (KTC), on the hypothalamic-pituitary-gonadal (HPG) axis of the Japanese medaka (Oryzias latipe) [corrected] were examined by use of real time PCR (RT-PCR) ..
  32. Rakhit A, Pantze M, Fettner S, Jones H, Charoin J, Riek M, et al. The effects of CYP3A4 inhibition on erlotinib pharmacokinetics: computer-based simulation (SimCYP) predicts in vivo metabolic inhibition. Eur J Clin Pharmacol. 2008;64:31-41 pubmed
    ..A drug-drug interaction study was therefore conducted for erlotinib and a potent CYP3A4 inhibitor, ketoconazole, in healthy male volunteers to evaluate the impact of CYP3A4 inhibition on erlotinib exposure...
  33. Zhang H, Wang K, Zhang G, Ho H, Gao A. Synergistic anti-candidal activity of tetrandrine on ketoconazole: an experimental study. Planta Med. 2010;76:53-61 pubmed publisher
    ..The study examined the synergism of tetrandrine (TET) on ketoconazole (KCZ) candidacidal activity...
  34. Patricelli A, Hardie R, McAnulty J. Cyclosporine and ketoconazole for the treatment of perianal fistulas in dogs. J Am Vet Med Assoc. 2002;220:1009-16 pubmed
    To evaluate efficacy and cost of using cyclosporine and ketoconazole for the treatment of perianal fistulas in dogs.
  35. O Neill T, Edwards G, Holloway S. Efficacy of combined cyclosporine A and ketoconazole treatment of anal furunculosis. J Small Anim Pract. 2004;45:238-43 pubmed
    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...
  36. Santa Rita R, Lira R, Barbosa H, Urbina J, de Castro S. Anti-proliferative synergy of lysophospholipid analogues and ketoconazole against Trypanosoma cruzi (Kinetoplastida: Trypanosomatidae): cellular and ultrastructural analysis. J Antimicrob Chemother. 2005;55:780-4 pubmed
    ..analogues (LPAs) edelfosine, ilmofosine and miltefosine with the ergosterol biosynthesis inhibitor ketoconazole against Trypanosoma cruzi...
  37. Ogasawara A, Kume T, Kazama E. Effect of oral ketoconazole on intestinal first-pass effect of midazolam and fexofenadine in cynomolgus monkeys. Drug Metab Dispos. 2007;35:410-8 pubmed
    ..MDZ) and fexofenadine (FEX), typical substrates for CYP3A and P-glycoprotein (P-gp), respectively, with ketoconazole (KTZ) as a potent dual CYP3A/P-gp inhibitor in cynomolgus monkeys. When MDZ or FEX was administered i.v...
  38. Rautemaa R, Richardson M, Pfaller M, Perheentupa J, Saxen H. Reduction of fluconazole susceptibility of Candida albicans in APECED patients due to long-term use of ketoconazole and miconazole. Scand J Infect Dis. 2008;40:904-7 pubmed publisher
    ..Significantly more y of usage of ketoconazole and miconazole preceded the isolation of strains with decreased susceptibility to fluconazole than susceptible ..
  39. Allqvist A, Miura J, Bertilsson L, Mirghani R. Inhibition of CYP3A4 and CYP3A5 catalyzed metabolism of alprazolam and quinine by ketoconazole as racemate and four different enantiomers. Eur J Clin Pharmacol. 2007;63:173-9 pubmed
    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...
  40. Shams Ghahfarokhi M, Shokoohamiri M, Amirrajab N, Moghadasi B, Ghajari A, Zeini F, et al. In vitro antifungal activities of Allium cepa, Allium sativum and ketoconazole against some pathogenic yeasts and dermatophytes. Fitoterapia. 2006;77:321-3 pubmed
    ..well as 35 strains of various dermatophyte species and compared with the activity of a known antifungal drug, ketoconazole (KTZ)...
  41. Furukawa S, Hayashi S, Usuda K, Abe M, Ogawa I. Histopathological effect of ketoconazole on rat placenta. J Vet Med Sci. 2008;70:1179-84 pubmed
    In order to investigate the morphological effects of ketoconazole on hypertrophied placentas, we examined the sequential histopathological changes in the placenta from rats exposed to ketoconazole...
  42. Van Roey J, Haxaire M, Kamya M, Lwanga I, Katabira E. Comparative efficacy of topical therapy with a slow-release mucoadhesive buccal tablet containing miconazole nitrate versus systemic therapy with ketoconazole in HIV-positive patients with oropharyngeal candidiasis. J Acquir Immune Defic Syndr. 2004;35:144-50 pubmed
    ..of miconazole nitrate mucoadhesive buccal tablet (n = 178) versus a 400-mg once-daily systemic regimen of ketoconazole (n = 179) in HIV-positive patients with oropharyngeal candidiasis...
  43. Das B, Madhukumar A, Anguiano J, Kim S, Sinz M, Zvyaga T, et al. Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR). Bioorg Med Chem Lett. 2008;18:3974-7 pubmed publisher
    ..In this context, there is a paucity of inhibitors directed toward activated PXR. Using prior observations with ketoconazole as a PXR inhibitor, the target compound 3 was synthesized from (s)-glycidol with overall 56% yield...
  44. Goel S, Cohen M, Cömezoğlu S, Perrin L, Andre F, Jayabalan D, et al. The effect of ketoconazole on the pharmacokinetics and pharmacodynamics of ixabepilone: a first in class epothilone B analogue in late-phase clinical development. Clin Cancer Res. 2008;14:2701-9 pubmed publisher
    ..metabolism by this cytochrome is clinically important, we did a clinical drug interaction study in humans using ketoconazole as an inhibitor of CYP3A4...
  45. Pyun M, Shin S. Antifungal effects of the volatile oils from Allium plants against Trichophyton species and synergism of the oils with ketoconazole. Phytomedicine. 2006;13:394-400 pubmed
    ..The combined effects of Allium oils with ketoconazole were tested by the checkerboard titer test. Among the tested oils, A. sativum for...
  46. Ferrando A, Wolfe R. Restoration of hormonal action and muscle protein. Crit Care Med. 2007;35:S630-4 pubmed
    ..To restore hormonal influence, clinicians should consider reestablishing anabolic stimuli and reducing catabolic stimuli. ..
  47. Chandel N, Aggarwal P, Minz M, Sakhuja V, Kohli K, Jha V. CYP3A5*1/*3 genotype influences the blood concentration of tacrolimus in response to metabolic inhibition by ketoconazole. Pharmacogenet Genomics. 2009;19:458-63 pubmed publisher
    b>Ketoconazole retards metabolic degradation of tacrolimus through its effect on the cytochrome P-450 enzyme system and allows reduction in treatment costs...
  48. Lim Y, Kuo S, Lai M, Huang J. 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. Pharmacogenet Genomics. 2009;19:11-24 pubmed publisher
    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...
  49. Duret C, Daujat Chavanieu M, Pascussi J, Pichard Garcia L, Balaguer P, Fabre J, et al. 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. Mol Pharmacol. 2006;70:329-39 pubmed
    ..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)..
  50. Segersten U, Björklund P, Hellman P, Akerstrom G, Westin G. Potentiating effects of nonactive/active vitamin D analogues and ketoconazole in parathyroid cells. Clin Endocrinol (Oxf). 2007;66:399-404 pubmed
    ..Effects of vitamin D analogues and ketoconazole on parathyroid hormone (PTH) secretion (radioimmunoassay) and PTH mRNA expression (reverse transcription-..
  51. Villeneuve D, Blake L, Brodin J, Greene K, Knoebl I, Miracle A, et al. Transcription of key genes regulating gonadal steroidogenesis in control and ketoconazole- or vinclozolin-exposed fathead minnows. Toxicol Sci. 2007;98:395-407 pubmed
    ..study evaluated changes in the expression of steroidogenesis-related genes in male fathead minnows exposed to ketoconazole (KTC) or vinclozolin (VZ) for 21 days...
  52. Borgers M, Degreef H. The role of ketoconazole in seborrheic dermatitis. Cutis. 2007;80:359-63 pubmed
    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 ..
  53. Gunt H, Kasting G. Effect of hydration on the permeation of ketoconazole through human nail plate in vitro. Eur J Pharm Sci. 2007;32:254-60 pubmed
    The impact of hydration on the permeation of the antifungal drug, ketoconazole, through excised human nails in vitro was evaluated in diffusion cell studies...