Fluconazole, D0870, and flucytosine treatment of disseminated Candida tropicalis infections in mice.
Graybill, J R, Najvar, L K, Holmberg, J D, Luther, M F
D0870 is a recently developed triazole with characteristics of a broad spectrum of activity and slow clearance by nonrenal mechanisms. Herein we have evaluated the efficacy of D0870, alone and...
Evaluation of SCH51048 in an experimental model of pulmonary aspergillosis.
Allendoerfer, R, Loebenberg, D, Rinaldi, M G, Graybill, J R
The efficacy of a novel triazole, SCH51048, was assessed with a murine model of pulmonary aspergillosis and was compared with those of SCH39304 and itraconazole. A wide range of doses of SCH51048 (5...
Liposomal amphotericin B therapy of murine histoplasmosis.
Liposomal amphotericin B (AmBisome) was compared with amphotericin B deoxycholate for the treatment of disseminated murine histoplasmosis. Liposomal amphotericin B was well tolerated and, milligram...
Graybill, J R, Najvar, L K, Holmberg, J D, Correa, A, Luther, M F
A series of fluconazole-susceptible and-fluconazole resistant Candida albicans fungal isolates were used to infect mice intravenously. Mice were treated with varying doses of fluconazole beginning...
Atkinson, B A, Bocanegra, R, Graybill, J R
An animal model of disseminated Mycobacterium haemophilum infection was utilized to compare treatment with azithromycin, ciprofloxacin, rifabutin, and the combination of clarithromycin with...
Four patients with cryptococcal meningitis were treated with amphotericin B colloidal dispersion because of nephrotoxicity from prior treatment with conventional amphotericin B. The limited...
Bleomycin therapy of experimental disseminated candidiasis in mice.
Graybill, J R, Bocanegra, R, Fothergill, A, Rinaldi, M G
Bleomycin, an antineoplastic agent, was found to be very effective in vitro against a variety of fungi, including Candida albicans. Mice were infected with C. albicans intravenously and then treated...
Barchiesi, F, Najvar, L K, Luther, M F, Scalise, G, Rinaldi, M G, Graybill, J R
Four strains of Candida albicans, isolated from two patients with AIDS who had undergone prolonged fluconazole therapy for oral candidiasis, were studied in a model of disseminated murine...
Effect of fluconazole on fungicidal activity of flucytosine in murine cryptococcal meningitis.
Larsen, R A, Bauer, M, Weiner, J M, Diamond, D M, Leal, M E, Ding, J C, ...
Both animal and in vitro studies have demonstrated that combinations of flucytosine with amphotericin B and with fluconazole have significantly improved activity against cryptococcal meningitis...
Combination therapy with fluconazole and flucytosine in the murine model of cryptococcal meningitis.
Nguyen, M H, Najvar, L K, Yu, C Y, Graybill, J R
This study elucidates the role of combined fluconazole and flucytosine as therapy for cryptococcosis in the murine model of meningitis. Three strains of Cryptococcus neoformans for which the range of...
Ding, J C, Bauer, M, Diamond, D M, Leal, M A, Johnson, D, Williams, B K, ...
We studied the effect of the severity of meningitis on the response to therapy with fluconazole and flucytosine in a murine model of cryptococcal meningitis. Meningitis was established by...
Treatment of murine disseminated candidiasis with L-743,872.
Graybill, J R, Najvar, L K, Luther, M F, Fothergill, A W
L-743,872 (M991), which is a pneumocandin derivative, was evaluated in a mouse model of disseminated candidiasis caused by a fluconazole-resistant isolate of Candida albicans. In immunocompetent mice...
Treatment of murine Candida krusei or Candida glabrata infection with L-743,872.
Graybill, J R, Bocanegra, R, Luther, M, Fothergill, A, Rinaldi, M J
L-743,872 is a broad-spectrum pneumocandin antifungal drug developed by Merck Research Co., and in the present work it was evaluated in vivo in murine models of Candida krusei and Candida glabrata...
Treatment of murine coccidioidal meningitis with SCH39304.
Defaveri, J, Sun, S H, Graybill, J R
The triazole SCH39304 was compared with itraconazole and fluconazole for treatment of murine coccidioidal meningitis. Mice were treated for 30 days with 1, 5, 10, or 30 mg of each drug per kg of body...
Efficacy of SCH39304 in murine cryptococcosis.
Restrepo, B I, Ahrens, J, Graybill, J R
Cryptococcal meningitis is increasing in frequency, in large part because of the advent of acquired immune deficiency syndrome. Using the murine cryptococcosis model, a new oral triazole, SCH39304,...
Adrenal response to corticotropin during therapy with itraconazole.
Phillips, P, Graybill, J R, Fetchick, R, Dunn, J F
Itraconazole is a triazole with a mechanism of action similar to that of ketoconazole. Endocrine side effects of ketoconazole, including impaired cortisol synthesis, have been well documented (A....
Pharmacology and toxicity of high-dose ketoconazole.
Sugar, A M, Alsip, S G, Galgiani, J N, Graybill, J R, Dismukes, W E, Cloud, G A, ...
One hundred sixty patients were entered in two multicenter protocols to receive 400 to 2,000 mg of ketoconazole once daily for nonmeningeal or meningeal coccidiodomycosis. For 24 h after...
Pharmacokinetics of itraconazole following oral administration to normal volunteers.
Hardin, T C, Graybill, J R, Fetchick, R, Woestenborghs, R, Rinaldi, M G, Kuhn, J G
The pharmacokinetics of itraconazole, an orally effective, broad-spectrum, systemic antifungal agent, were evaluated in five healthy male volunteers. Each subject was studied on days 1 and 15 at the...
Sensitive bioassay for ketoconazole in serum and cerebrospinal fluid.
Jorgensen, J H, Alexander, G A, Graybill, J R, Drutz, D J
Ketoconazole is a broad-spectrum antifungal agent which appears promising for treatment of a variety of systemic mycoses. Pharmacokinetic studies are limited due to a lack of readily available...
Comparative activities of Bay n7133, ICI 153,066, and ketoconazole in murine cryptococcosis.
Graybill, J R, Kaster, S R, Drutz, D J
Two new antifungal triazoles, BAY n7133 and ICI 153,066, were compared with ketoconazole in treatment of mice challenged intraperitoneally with Cryptococcus neoformans. At high challenge doses,...
Valero, G, Moreno, F, Graybill, J R
After 2 weeks of intravenous challenge with Mycobacterium simiae, ICR outbred mice were treated with clarithromycin, ofloxacin, or clarithromycin plus ethambutol for 4 weeks. All three therapy groups...
Allendoerfer, R, Yates, R R, Marquis, A J, Loebenberg, D, Rinaldi, M G, Graybill, J R
SCH 39304 (304) and its isomers, SCH 42426 (426) and SCH 42427 (427), are new orally administered antifungal azole derivatives. In this study, we compared the efficacy of 304 with that of 426 and 427...
Use of high-dose fluconazole as salvage therapy for cryptococcal meningitis in patients with AIDS.
Berry, A J, Rinaldi, M G, Graybill, J R
Eight patients with AIDS were treated orally with 800 mg of fluconazole daily for cryptococcal meningitis for a mean duration of 4.5 months. Previous antifungal treatment had failed for all of the...
High-dose itraconazole in the treatment of severe mycoses.
Sharkey, P K, Rinaldi, M G, Dunn, J F, Hardin, T C, Fetchick, R J, Graybill, J R
Eight patients with systemic mycoses and with prior treatment failures were treated with itraconazole (600 mg/day) for a mean duration of 5.5 months. All six patients without AIDS experienced...
Combined therapy with fluconazole and flucytosine in murine cryptococcal meningitis.
Allendoerfer, R, Marquis, A J, Rinaldi, M G, Graybill, J R
To assess the possible beneficial effects of combined therapy (fluconazole and flucytosine) in the treatment of cryptococcal meningitis in the immunocompromised host, we compared therapy with...
Treatment of murine cryptococcal meningitis with an SCH 39304-amphotericin B combination.
Albert, M M, Graybill, J R, Rinaldi, M G
Cryptococcal meningitis was induced in BALB/c mice by intracerebral infection with Cryptococcus neoformans. Drug therapy was initiated 1 day later, with mice receiving amphotericin B (AMB), SCH...
Hardin, T C, Sharkey, P K, Lam, Y F, Wallace, J E, Rinaldi, M G, Graybill, J R
The pharmacokinetics of SCH-39304, an investigational, orally active, broad-spectrum antifungal agent, were evaluated in 17 adult, human immunodeficiency virus-positive males. Patients were studied...
Treatment of disseminated Torulopsis glabrata infection with DO870 and amphotericin B.
Atkinson, B A, Bocanegra, R, Colombo, A L, Graybill, J R
Torulopsis glabrata, an opportunist pathogen in immunosuppressed patients, is resistant to many antifungal agents, and there are no established treatment regimens for this organism. The mouse model...
Transfer of protective immunity in murine histoplasmosis by a CD4+ T-cell clone.
Allendoerfer, R, Magee, D M, Deepe, G S, Graybill, J R
We have reported that a murine Histoplasma capsulatum-reactive CD4+ T-cell line and clones thereof did not adoptively transfer protection against H. capsulatum infection in normal or...
Cyclophosphamide effects on murine cryptococcosis.
BALB/c mice were given cyclophosphamide and challenged with Cryptococcus neoformans. Delayed-type hypersensitivity was transiently depressed, and survival was either unaffected or shortened by...
Histoplasma capsulatum infection in nude mice.
Williams, D M, Graybill, J R, Drutz, D J
Congenitally athymic nude (nu/nu) mice, when injected intraperitoneally with Histoplasma capsulatum, developed a rapidly fatal disseminated infection characterized by heavy parasitization of...
Fluconazole, D0870, and flucytosine treatment of disseminated Candida tropicalis infections in mice.
Graybill, J R, Najvar, L K, Holmberg, J D, Luther, M F
D0870 is a recently developed triazole with characteristics of a broad spectrum of activity and slow clearance by nonrenal mechanisms. Herein we have evaluated the efficacy of D0870, alone and...
Evaluation of SCH51048 in an experimental model of pulmonary aspergillosis.
Allendoerfer, R, Loebenberg, D, Rinaldi, M G, Graybill, J R
The efficacy of a novel triazole, SCH51048, was assessed with a murine model of pulmonary aspergillosis and was compared with those of SCH39304 and itraconazole. A wide range of doses of SCH51048 (5...
Liposomal amphotericin B therapy of murine histoplasmosis.
Liposomal amphotericin B (AmBisome) was compared with amphotericin B deoxycholate for the treatment of disseminated murine histoplasmosis. Liposomal amphotericin B was well tolerated and, milligram...
Graybill, J R, Najvar, L K, Holmberg, J D, Correa, A, Luther, M F
A series of fluconazole-susceptible and-fluconazole resistant Candida albicans fungal isolates were used to infect mice intravenously. Mice were treated with varying doses of fluconazole beginning...
Atkinson, B A, Bocanegra, R, Graybill, J R
An animal model of disseminated Mycobacterium haemophilum infection was utilized to compare treatment with azithromycin, ciprofloxacin, rifabutin, and the combination of clarithromycin with...
Four patients with cryptococcal meningitis were treated with amphotericin B colloidal dispersion because of nephrotoxicity from prior treatment with conventional amphotericin B. The limited...
Bleomycin therapy of experimental disseminated candidiasis in mice.
Graybill, J R, Bocanegra, R, Fothergill, A, Rinaldi, M G
Bleomycin, an antineoplastic agent, was found to be very effective in vitro against a variety of fungi, including Candida albicans. Mice were infected with C. albicans intravenously and then treated...
Barchiesi, F, Najvar, L K, Luther, M F, Scalise, G, Rinaldi, M G, Graybill, J R
Four strains of Candida albicans, isolated from two patients with AIDS who had undergone prolonged fluconazole therapy for oral candidiasis, were studied in a model of disseminated murine...
Effect of fluconazole on fungicidal activity of flucytosine in murine cryptococcal meningitis.
Larsen, R A, Bauer, M, Weiner, J M, Diamond, D M, Leal, M E, Ding, J C, ...
Both animal and in vitro studies have demonstrated that combinations of flucytosine with amphotericin B and with fluconazole have significantly improved activity against cryptococcal meningitis...
Combination therapy with fluconazole and flucytosine in the murine model of cryptococcal meningitis.
Nguyen, M H, Najvar, L K, Yu, C Y, Graybill, J R
This study elucidates the role of combined fluconazole and flucytosine as therapy for cryptococcosis in the murine model of meningitis. Three strains of Cryptococcus neoformans for which the range of...
Ding, J C, Bauer, M, Diamond, D M, Leal, M A, Johnson, D, Williams, B K, ...
We studied the effect of the severity of meningitis on the response to therapy with fluconazole and flucytosine in a murine model of cryptococcal meningitis. Meningitis was established by...
Treatment of murine disseminated candidiasis with L-743,872.
Graybill, J R, Najvar, L K, Luther, M F, Fothergill, A W
L-743,872 (M991), which is a pneumocandin derivative, was evaluated in a mouse model of disseminated candidiasis caused by a fluconazole-resistant isolate of Candida albicans. In immunocompetent mice...
Treatment of murine Candida krusei or Candida glabrata infection with L-743,872.
Graybill, J R, Bocanegra, R, Luther, M, Fothergill, A, Rinaldi, M J
L-743,872 is a broad-spectrum pneumocandin antifungal drug developed by Merck Research Co., and in the present work it was evaluated in vivo in murine models of Candida krusei and Candida glabrata...
Treatment of murine coccidioidal meningitis with SCH39304.
Defaveri, J, Sun, S H, Graybill, J R
The triazole SCH39304 was compared with itraconazole and fluconazole for treatment of murine coccidioidal meningitis. Mice were treated for 30 days with 1, 5, 10, or 30 mg of each drug per kg of body...
Efficacy of SCH39304 in murine cryptococcosis.
Restrepo, B I, Ahrens, J, Graybill, J R
Cryptococcal meningitis is increasing in frequency, in large part because of the advent of acquired immune deficiency syndrome. Using the murine cryptococcosis model, a new oral triazole, SCH39304,...
Adrenal response to corticotropin during therapy with itraconazole.
Phillips, P, Graybill, J R, Fetchick, R, Dunn, J F
Itraconazole is a triazole with a mechanism of action similar to that of ketoconazole. Endocrine side effects of ketoconazole, including impaired cortisol synthesis, have been well documented (A....
Pharmacology and toxicity of high-dose ketoconazole.
Sugar, A M, Alsip, S G, Galgiani, J N, Graybill, J R, Dismukes, W E, Cloud, G A, ...
One hundred sixty patients were entered in two multicenter protocols to receive 400 to 2,000 mg of ketoconazole once daily for nonmeningeal or meningeal coccidiodomycosis. For 24 h after...
Pharmacokinetics of itraconazole following oral administration to normal volunteers.
Hardin, T C, Graybill, J R, Fetchick, R, Woestenborghs, R, Rinaldi, M G, Kuhn, J G
The pharmacokinetics of itraconazole, an orally effective, broad-spectrum, systemic antifungal agent, were evaluated in five healthy male volunteers. Each subject was studied on days 1 and 15 at the...
Sensitive bioassay for ketoconazole in serum and cerebrospinal fluid.
Jorgensen, J H, Alexander, G A, Graybill, J R, Drutz, D J
Ketoconazole is a broad-spectrum antifungal agent which appears promising for treatment of a variety of systemic mycoses. Pharmacokinetic studies are limited due to a lack of readily available...
Comparative activities of Bay n7133, ICI 153,066, and ketoconazole in murine cryptococcosis.
Graybill, J R, Kaster, S R, Drutz, D J
Two new antifungal triazoles, BAY n7133 and ICI 153,066, were compared with ketoconazole in treatment of mice challenged intraperitoneally with Cryptococcus neoformans. At high challenge doses,...
Valero, G, Moreno, F, Graybill, J R
After 2 weeks of intravenous challenge with Mycobacterium simiae, ICR outbred mice were treated with clarithromycin, ofloxacin, or clarithromycin plus ethambutol for 4 weeks. All three therapy groups...
Allendoerfer, R, Yates, R R, Marquis, A J, Loebenberg, D, Rinaldi, M G, Graybill, J R
SCH 39304 (304) and its isomers, SCH 42426 (426) and SCH 42427 (427), are new orally administered antifungal azole derivatives. In this study, we compared the efficacy of 304 with that of 426 and 427...
Use of high-dose fluconazole as salvage therapy for cryptococcal meningitis in patients with AIDS.
Berry, A J, Rinaldi, M G, Graybill, J R
Eight patients with AIDS were treated orally with 800 mg of fluconazole daily for cryptococcal meningitis for a mean duration of 4.5 months. Previous antifungal treatment had failed for all of the...
High-dose itraconazole in the treatment of severe mycoses.
Sharkey, P K, Rinaldi, M G, Dunn, J F, Hardin, T C, Fetchick, R J, Graybill, J R
Eight patients with systemic mycoses and with prior treatment failures were treated with itraconazole (600 mg/day) for a mean duration of 5.5 months. All six patients without AIDS experienced...
Combined therapy with fluconazole and flucytosine in murine cryptococcal meningitis.
Allendoerfer, R, Marquis, A J, Rinaldi, M G, Graybill, J R
To assess the possible beneficial effects of combined therapy (fluconazole and flucytosine) in the treatment of cryptococcal meningitis in the immunocompromised host, we compared therapy with...
Treatment of murine cryptococcal meningitis with an SCH 39304-amphotericin B combination.
Albert, M M, Graybill, J R, Rinaldi, M G
Cryptococcal meningitis was induced in BALB/c mice by intracerebral infection with Cryptococcus neoformans. Drug therapy was initiated 1 day later, with mice receiving amphotericin B (AMB), SCH...
Hardin, T C, Sharkey, P K, Lam, Y F, Wallace, J E, Rinaldi, M G, Graybill, J R
The pharmacokinetics of SCH-39304, an investigational, orally active, broad-spectrum antifungal agent, were evaluated in 17 adult, human immunodeficiency virus-positive males. Patients were studied...
Treatment of disseminated Torulopsis glabrata infection with DO870 and amphotericin B.
Atkinson, B A, Bocanegra, R, Colombo, A L, Graybill, J R
Torulopsis glabrata, an opportunist pathogen in immunosuppressed patients, is resistant to many antifungal agents, and there are no established treatment regimens for this organism. The mouse model...
Transfer of protective immunity in murine histoplasmosis by a CD4+ T-cell clone.
Allendoerfer, R, Magee, D M, Deepe, G S, Graybill, J R
We have reported that a murine Histoplasma capsulatum-reactive CD4+ T-cell line and clones thereof did not adoptively transfer protection against H. capsulatum infection in normal or...
Cyclophosphamide effects on murine cryptococcosis.
BALB/c mice were given cyclophosphamide and challenged with Cryptococcus neoformans. Delayed-type hypersensitivity was transiently depressed, and survival was either unaffected or shortened by...
Histoplasma capsulatum infection in nude mice.
Williams, D M, Graybill, J R, Drutz, D J
Congenitally athymic nude (nu/nu) mice, when injected intraperitoneally with Histoplasma capsulatum, developed a rapidly fatal disseminated infection characterized by heavy parasitization of...
Variability of sequential studies of lymphocyte blastogenesis in normal adults.
Sixteen healthy adults had serial studies of delayed-type skin test reactivity and in vitro lymphocyte blastogenesis to several antigens over a period of 7 months. In many subjects blastogenesis...