The effect of ketoconazole on growth, sterol composition, in vitro sterol biosynthesis and P450-CO complex formation and its interaction with microsomal P450 was determined. On solid medium and in liquid medium ketoconazole inhibited Aspergillus fumigatus growth completely at 5 x 10(-5) M and 50% of the growth at 1.3 x 10(-5) M and 2.1 x 10(-5) M respectively. A close relationship between accum...

Prior to the development of ketoconazole, the treatment of systemic histoplasmosis and blastomycosis was limited to AMB. The convenience of oral dosing, combined with avoidance of the significant toxicities associated with AMB, make ketoconazole an attractive alternative for the treatment of selected forms of histoplasmosis and blastomycosis. Although high-dose (800 mg/day) ketoconazole is gene...

Background: Tinea versicolor is a common superficial mycosis, which is caused by lipophilic yeasts, malessezia furfur. It is a chronic and recurrent skin disease. It occurs most commonly in young post-pubertal people and in hot and humid climates (North and south provinces of Iran). Objective: Comparison of effects of ketoconazole 2% shampoo (Shafa Lab) with selenium sulfide 2.5% shampoo on tin...

The effect of P-glycoprotein (Pgp) and/or CYP3A on the disposition of xenobiotics has been extensively investigated and is often of interest during drug discovery lead optimization. We have previously described a monkey pharmacokinetic screen to rapidly estimate absorption and first-pass extraction. In the present work, this monkey screen has been expanded to include an assessment of Pgp/CYP3A ...

Eight healthy adults were given single oral doses of ketoconazole (200, 400, 600, and 800 mg) in the fasting state and with a standard breakfast at weekly intervals according to a balanced block design. Concentrations in serum were measured up to 32 h after the dose. Food did not reduce ketoconazole absorption or significantly alter peak ketoconazole concentrations in serum, though there was a ...

The antifungal activity of orally active SM-4470, (R)-3-(n-butylthio)-2-(2,4-dichlorophenyl)-1-(imidazole-1-yl)-2-propanol hydrochloride, was compared with that of ketoconazole. SM-4470 showed twofold-higher activity than ketoconazole in the oral treatment of systemic infection with Candida albicans in mice. In addition, SM-4470 was effective against aspergillosis in mice, but ketoconazole was ...

INTRODUCTION Mifepristone, a competitive glucocorticoid receptor antagonist approved for Cushing syndrome, and ketoconazole, an antifungal and steroidogenesis inhibitor, are both inhibitors of and substrates for cytochrome P450 (CYP3A4). This study evaluated the pharmacokinetic effects of concomitant ketoconazole, a strong CYP3A4 inhibitor, on mifepristone. METHODS In an open-label, two-perio...

Preclinical and clinical data support the importance of signaling via the androgen receptor even in the setting of castration-resistant prostate cancer. However, the role of additional hormonal manipulations in patients progressing on cytotoxic chemotherapy has not been well defined. Recently, the novel lyase inhibitor, abiraterone acetate, has shown activity in patients with docetaxel-refracto...