Hepatic reactions associated with ketoconazole in the United Kingdom.

Lake‐Bakaar, Gerond; Scheuer, P. J.; Sherlock, Sheila

doi:10.1136/bmj.294.6569.419

Cited by 156 publications

(55 citation statements)

References 14 publications

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“…Interestingly, the endocrine effects of ketoconazole have suggested a new use for the drug: the treatment of prostatic cancer (6, 305). Excellent reviews on hepatotoxicity (166) and endocrine effects of ketoconazole have been published recently (84,280,281).…”

Section: Ketoconazolementioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

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Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

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Section: Ketoconazolementioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

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“…In 1996, Njar et al [20,26] reported the first steroidal inhibitors of CYP17 bearing a heterocyclic moiety bound to C17 by a nitrogen atom, among which the imidazolyl derivative 1 was found to be the most promising [20][21][22][23][26][27][28][29]. Later, in 2005, the same group reported the synthesis of galeterone 2 and its Δ 4 -3-keto derivative [23][24][25][29][30][31], where compound 2 is currently undergoing Phase I/II clinical trials for the treatment of chemotherapy-naive CRPC [26,27,[32][33]. However, patients suffering from CRPC can clearly benefit from the newly approved drug abiraterone acetate (Zytiga) 3 [28,29,34,35].…”

Section: Introductionmentioning

confidence: 99%

“…Recently, several steroidal compounds have been synthesized and displayed a key role in a therapeutic strategy for treating advanced prostate cancer (PC) [23][24][25]. In 1996, Njar et al [20,26] reported the first steroidal inhibitors of CYP17 bearing a heterocyclic moiety bound to C17 by a nitrogen atom, among which the imidazolyl derivative 1 was found to be the most promising [20][21][22][23][26][27][28][29].…”

Section: Introductionmentioning

confidence: 99%

Exploration of new 3α-pregnenolone ester analogues via Mitsunobu reaction, their anti-HIV activity and molecular modeling study

2015

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A new series of (5-pregnen-20-on-3α-yl)-substituted-benzoate analogues (10-13), (5-pregnene-20-on-3α-yl)-3-(substituted)acrylate derivatives (17-19) as well as the (17-(2-acetoxyacetyl)pregen-3α-yl)-3,4,5-trihydroxybenzoate (21) were synthesized from the β-pregenenolone scaffolds, by applying Mitsunobu reaction. All new compounds were characterized by 1 H, 13 C and 2D NMR spectroscopy. The inversion in configuration at C-3 during the formation of α-ester analogues was confirmed by NOESY NMR spectroscopy. The new compounds were evaluated for their in vitro antiviral activity against the replication of HIV-1 and HIV-2 in MT-4 cells. Compounds 18 showed an EC50 value of >1.95 mg/mL. In addition, preliminary structure-activity relationship and molecular modeling of compound 18 has been studied.

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“…Other options include secondary hormonal therapy using mainly ketoconazole due to its ability to inhibit cytochrome P450 17-hydroxylase C 17,20 -lyase (CYP17), one of the enzymes responsible for the biosynthesis of androgen precursors in the human body (Moreira et al, 2008). Despite its efficacy and ease of administration, ketoconazole bears several side effects (De Felice et al, 1981, Lake-Bakaar et al, 1987. Patients with CRPC are currently treated with docetaxel ( Fig.…”

Section: Prostate Cancer Worldwidementioning

confidence: 99%