Ketoconazole is an imidazole-containing small molecule inhibitor of cytochrome P-450-dependent steps in the biosynthesis of steroid hormones; also inhibits TXA Synthase (thromboxane synthetase) and 5-LO (5-lipoxygenase) activity. Ketoconazole exhibits antimetastatic, antineoplastic, and antipsoriatic activity. Inhibition of 5-LO (5-lipoxygenase) by Ketoconazole interrupts arachidonic acid (sc-200770)-derived leukotriene production, which was correlated to a suppression of leukotriene-mediated anaphylactic bronchoconstriction in guinea pigs. Ketoconazole is described as reducing platelet cellular levels of thromboxane A2, suppressing thromboxane A2-mediated increase of microvascular permeability in response to ischemia insults. Ketoconazole produces an antiandrogen effect through inhibition of adrenocorticoid biosynthesis, suppressing the adrenal secretion of androgens and attenuating cortisol response. Ketoconazole is an inhibitor of CYP17A1, CYP3A4 and CYP3A5.
1. Lelcuk, S., et al. 1984. J Trauma. 24: 393-396. PMID: 6325720
2. Lelcuk, S., et al. 1985. Ann. Surg. 202: 642-646. PMID: 3840349
3. Lambert, A., et al. 1986. Biochem. Pharmacol. 35: 3999-4004. PMID: 3022746
4. Beetens, J.R., et al. 1986. Biochem. Pharmacol. 35: 883-891. PMID: 3006695
5. Boscaro, M., et al. 1987. Horm. Metab. Res. Suppl. 16: 60-62. PMID: 2832292
6. Nardone, P.A., et al. 1988. J. Surg. Res. 44: 425-429. PMID: 3361885
7. Ward, A.S., et al. 1998. Behav Pharmacol. 9: 577-586. PMID: 9862083
8. Richie, J.P. 1999. Urology. 54: 15-18. PMID: 10606279
9. Chaudhary, U.B., et al. 2005. Can J Urol. 12: 2666-2676. PMID: 16011813
See how others have used Ketoconazole. Click on the entry to view the PubMed entry .
PMID: # 28461309
Hargrove, TY. et al. 2017. Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity. Antimicrob. Agents Chemother.. 61:
PMID: # 25652406
Cunningham, D. et al. 2015. Analysis of hedgehog signaling in cerebellar granule cell precursors in a conditional Nsdhl allele demonstrates an essential role for cholesterol in postnatal CNS development. Hum. Mol. Genet.. 24: 2808-25.
PMID: # 20146553
Patel, MR. et al. 2011. Investigating effect of microemulsion components: In vitro permeation of ketoconazole. Pharm Dev Technol. 16: 250-258.
PMID: # 20228983
Khozeimeh, F. et al. 2010. Comparative evaluation of ketoconazole tablet and topical ketoconazole 2% in orabase in treatment of Candida-infected denture stomatitis. J Contemp Dent Pract. 11: 017-024.
PMID: # 20346873
Seneca, N. et al. 2010. Effects of ketoconazole on the biodistribution and metabolism of [11C]loperamide and [11C]N-desmethyl-loperamide in wild-type and P-gp knockout mice. Nucl. Med. Biol.. 37: 335-345.
PMID: # 20233203
Shin, KH. et al. 2010. Effect of ketoconazole on the pharmacokinetics of udenafil in healthy Korean subjects. Br J Clin Pharmacol. 69: 307-310.
PMID: # 20337383
Morsy, MA. et al. 2009. Electron paramagnetic resonance method for the quantitative assay of ketoconazole in pharmaceutical preparations. Anal. Chem.. 81: 6991-6995.
PMID: # 2677377
Van Wauwe, JP. et al. 1989. Is there a case for P-450 inhibitors in cancer treatment? J. Med. Chem.. 32: 2231-2239.
PMID: # 3361885
Nardone, PA. et al. 1988. Ketoconazole: a thromboxane synthetase and 5-lipoxygenase inhibitor with antimetastatic activity in B16-F10 melanoma. J. Surg. Res.. 44: 425-429.
PMID: # 2832292
Boscaro, M. et al. 1987. ACTH response to corticotropin releasing hormone in Cushing's disease before and after ketoconazole: in vivo and in vitro studies. Horm. Metab. Res. Suppl.. 16: 60-62.
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