Licensed by Pfizer Catalog No.S1331 Synonyms: UK 49858
Molecular Weight(MW): 306.27
Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
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|Description||Fluconazole is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.|
Fluconazole in combination with amphotericin B (AmB) has a synergistic effect on C. albicans planktonic cells but does not alter AmB activity against biofilms. Fluconazole and caspofungin have an antagonistic effect against biofilms but not with planktonic cells. Fluconazole-mediated membrane perturbation (due to inhibition of ergosterol biosynthesis) increases calcineurin inhibitor intracellular concentrations. Fluconazole treatment significantly reduces levels of ergosterol within the cell in C. albicans planktonic cells, leading to cell membrane perturbation.  Fluconazole activity is less sensitive to acidic medium than is that of ketoconazole. Fluconazole is approximately 16-fold less active than ketoconazole against 35 representative isolates of C. albicans at physiologic pH.  Fluvastatin, a cholesterol-lowering drug, exhibits minimal activity (MICs of 64 to >128 mg/mL) against Candida species and Cryptococcus neoformans. Fluconazole combined with itraconazole exhibits potent activities against C. albicans, C. tropicalis, C. parapsilosis, and C. neoformans, including flucon- azole-resistant strains of C. albicans and C. tropicalis. 
|In vivo||Fluconazole is very effective in prolonging survival of rats infected with a representative candidal strain.  Fluconazole has a dramatic effect on the fungicidal activity of flucytosine in murine cryptococcal meningitis. Fluconazole combined with flucytosine and amphotericin B have significantly improved activity against cryptococcal meningitis compared with the activity of each drug used alone. |
-  Uppuluri P, et al. Antimicrob Agents Chemother, 2008, 52(3), 1127-1132.
-  Rogers TE, et al. Antimicrob Agents Chemother, 1986, 30(3), 418-422.
-  Chin NX, et al. Antimicrob Agents Chemother, 1997, 41(4), 850-852.
|In vitro||DMSO||61 mg/mL (199.17 mM)|
|Ethanol||61 mg/mL (199.17 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02733432||Completed||Candidiasis Vulvovaginal|Mycoses|Yeast Infection|Moniliasis Vulvovaginal|Vaginitis Monilial||Cidara Therapeutics Inc.||June 8 2016||Phase 2|
|NCT03451110||Completed||Healthy Subjects||Eisai Inc.|Purdue Pharma LP||February 5 2018||Phase 1|
|NCT01806623||Completed||Vulvovaginal Candidiasis||Pfizer||March 5 2013||Phase 3|
|NCT01307579||Completed||Acute Myeloid Leukemia|Adult Acute Megakaryoblastic Leukemia|Adult Acute Monoblastic Leukemia|Adult Acute Monocytic Leukemia|Adult Acute Myeloid Leukemia in Remission|Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With Maturation|Adult Acute Myeloid Leukemia With Minimal Differentiation|Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11|Adult Acute Myeloid Leukemia With t(8;21); (q22; q22.1); RUNX1-RUNX1T1|Adult Acute Myeloid Leukemia With t(9;11)(p22.3;q23.3); MLLT3-KMT2A|Adult Acute Myeloid Leukemia Without Maturation|Adult Acute Myelomonocytic Leukemia|Adult Erythroleukemia|Adult Pure Erythroid Leukemia|Alkylating Agent-Related Acute Myeloid Leukemia|Childhood Acute Erythroid Leukemia|Childhood Acute Megakaryoblastic Leukemia|Childhood Acute Monoblastic Leukemia|Childhood Acute Monocytic Leukemia|Childhood Acute Myeloid Leukemia in Remission|Childhood Acute Myeloid Leukemia With Maturation|Childhood Acute Myeloid Leukemia With Minimal Differentiation|Childhood Acute Myeloid Leukemia Without Maturation|Childhood Acute Myelomonocytic Leukemia|Fungal Infection|Myeloid Neoplasm|Neutropenia|Recurrent Adult Acute Myeloid Leukemia|Recurrent Childhood Acute Myeloid Leukemia|Secondary Acute Myeloid Leukemia|Untreated Adult Acute Myeloid Leukemia|Untreated Childhood Myeloid Neoplasm||Children''s Oncology Group|National Cancer Institute (NCI)||April 4 2011||Phase 3|
|NCT02663674||Suspended||Coccidioidomycosis||National Institute of Allergy and Infectious Diseases (NIAID)||December 29 2015||Phase 4|
|NCT03028103||Recruiting||Diffuse Large B Cell Lymphoma|Primary Mediastinal Lymphoma|Mantle Cell Lymphoma|Advanced Solid Tumor|Marginal Zone Lymphoma||Epizyme Inc.||March 27 2017||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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